|
T11428
|
Glyco-Obeticholic acid
|
FXR |
Metabolism |
|
Glyco-obeticholic acid 是一种牛磺酸的特性代谢物。Obeticholic Acid 是口服具有活性的法尼样 X 受体激动剂。 |
|
T23147
|
Phaclofen
3-Amino-2-(4-chlorophenyl)propanephosphonic acid
|
GABA Receptor |
Membrane transporter/Ion channel;
Neuroscience |
|
Phaclofen (3-Amino-2-(4-chlorophenyl)propanephosphonic acid) 是一种选择性 GABAB receptor 拮抗剂，可部分拮抗（-）-巴氯芬的镇静作用，可逆地拮抗巴氯芬或GABA对豚鼠回肠和远端结肠胆碱能抽搐反应的抑制，可用于研究神进系统疾病。 |
|
TP1819L
|
Substance P 1-9 aceate
|
Neurotensin Receptor |
GPCR/G Protein |
|
Substance P 1-9 aceate 是九肽，可减少豚鼠回肠和膀胱对 P 物质的失活。 |
|
T14326
|
AS-35
|
Leukotriene Receptor |
GPCR/G Protein |
|
AS-35 是一种可口服且具有选择性和高效性的 leukotrienes 拮抗剂，抑制 LTC4，LTD4 和 LTE4 诱导的回肠收缩。AS-35 具有抗过敏作用，抑制白三烯合成。 |
|
T12756
|
ROS 234 dioxalate
|
Histamine Receptor |
GPCR/G Protein;
Immunology/Inflammation;
Neuroscience |
|
ROS 234 dioxalate is a potent antagonist of H3(pKB of 9.46 for Guinea-pig ileum H3-receptor) |
|
T33449
|
ML 1035
ML103,ML-1035
|
Others |
Others |
|
ML 1035 is a benzamide that elicits contractions from guinea-pig non-stimulated ileum. |
|
T23829
|
Btm 1042
Btm1042,Btm-1042
|
Others |
Others |
|
Btm 1042 is an antispasmodic drug. It has been found to depress twitch responses in the ileum of guinea pigs. |
|
T27140
|
Delequamine HCl
RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197
|
Others |
Others |
|
Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72). |
|
T37494
|
11-trans Leukotriene E4
11-trans Leukotriene E4
|
Others |
Others |
|
Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans LTE4 is equipotent to LTE4 in contracting guinea pig ileum. |
|
T8437
|
3-(4-prop-2-en-1-ylpiperazin-1-yl)quinox
|
Others |
Others |
|
3-(4-prop-2-en-1-ylpiperazin-1-yl)quinox 拮抗 2-methyl-5-HT 诱导的豚鼠回肠收缩。 |
|
T70688
|
S 0960
|
Others |
Others |
|
S 0960 is a dimeric bile acid analogue that acts as a specific inhibitor of the apical sodium-dependent bile salt transporter (ASBT) in the ileum. |
|
TP1171
|
Apraglutide TFA (1295353-98-8 free base)
Apraglutide TFA,FE 203799e (TFA)
|
|
|
|
Apraglutide TFA (FE 203799 TFA), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum. |
|
TP1988
|
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
|
|
|
|
Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively) |
|
TP1819
|
Substance P (1-9)
|
|
|
|
Substance P (1-9) is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder. Subtance P is responsible for a number of excitatory effects on both central and peripheral neurons. |
|
TP2012
|
JMV 449
|
|
|
|
Potent, metabolically stable neurotensin receptor agonist peptide (IC50 = 0.15 nM for inhibition of [125I]-NT binding to neonatal mouse brain; EC50 = 1.9 nM for contraction of guinea pig ileum). Produces long-lasting hypothermic, neuroprotective and analg |
|
T71935
|
WIN 66306
|
Others |
Others |
|
WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner. |
|
T69126
|
Clofeverine (free base)
|
Others |
Others |
|
Clofeverine (free base) is a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine. |
|
T37492
|
11-trans Leukotriene C4
11-trans Leukotriene C4
|
Others |
Others |
|
11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ... |
|
T37652
|
5(S),6(R)-DiHETE
|
Others |
Others |
|
5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM. |
|
TP2075
|
Bombinakinin M
|
|
|
|
Potent bradykinin receptor agonist. Highly selective for mammalian arterial smooth muscle bradykinin receptors, displaying ~ 50-fold greater potency than bradykinin. Elicits dose-dependent contractile effects in smooth muscle of guinea pig ileum (EC50 = 4 |
|
T37493
|
11-trans Leukotriene D4
11-trans Leukotriene D4
|
Others |
Others |
|
11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guinea pig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea. |
|
T78563
|
[Leu13]-Motilin
KW-5139
|
Motilin Receptor |
GPCR/G Protein |
|
[Leu13]-Motilin (KW-5139) 为motilin类似物，能够刺激家兔胃肠运动，并在体外以浓度依赖性方式引起胃窦、十二指肠、空肠、回肠以及降结肠的收缩。 |
|
T69324
|
Clofeverine hydrochloride
|
Others |
Others |
|
Clofeverine hydrochloride is the salt form of Clofeverine (free base), a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine. |
|
T83497
|
[D-Pro2,D-Phe7,D-Trp9] Substance P
|
|
|
|
[D-Pro2,D-Phe7,D-Trp9]Substance P为Substance P的模拟物，并充当其抑制剂，能间接收缩豚鼠回肠。 |
|
T81079
|
Substance P (2-11)
|
|
|
|
Substance P (2-11)为P物质（SP）片段肽，具有对豚鼠回肠产生收缩活性的特性。同时，Substance P (2-11)能够抑制3H SP在BBMEC单分子层中的渗透。 |
|
T81078
|
Substance P (3-11)
|
|
|
|
Substance P (3-11)，作为P 物质 (SP) 的片段肽，具备穿透血脑屏障的能力，且对豚鼠回肠显示出收缩活性。 |
|
T76001
|
Apraglutide TFA
|
|
|
|
Apraglutide TFA (FE 203799 TFA) 是一种合成的、含33个氨基酸的肽类药物，为长效GLP-2类似物。它能在全回肠切除后导致的新生短肠综合征小猪中增强适应性和线性肠生长。 |
|
T60340
|
ROS 234
|
Others |
Others |
|
ROS 234 is a highly effective H3 antagonist, demonstrating a strong binding affinity (pK B) of 9.46 for the Guinea-pig ileum H3 receptor and a pKi of 8.90 for the Rat cerebral cortex H3 receptor. Additionally, it exhibits an ex vivo ED50 of 19.12 mg/kg (ip) in the Rat cerebral cortex. It should be noted that ROS 234 demonstrates limited central access, as reported in [1] and [2]. |
|
T26770
|
Bencycloquidium Bromide
BCQB
|
Others |
Others |
|
Bencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is un... |
|
T84590
|
17-phenyl trinor Prostaglandin E2
17-phenyl trinor PGE2
|
Others |
Others |
|
17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg/kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2. |
|
TP2012L
|
JMV 449 acetate(139026-66-7 Free bsae)
|
|
|
|
JMV 449 acetate(139026-66-7 Free bsae) 是一种有效的、代谢稳定的神经降压素受体激动剂肽（抑制[125I]-NT与新生小鼠大脑的结合的IC50 = 0.15 nM；对于豚鼠收缩的EC50 = 1.9 nM 回肠）。 JMV 449 acetate 在小鼠体内中枢给药后产生持久的低温、神经保护和镇痛作用。 |
|
T10294
|
AM9405
|
5-HT Receptor |
GPCR/G Protein;
Neuroscience |
|
AM9405是一种新型的外周活性大麻素1型 (CB1)和5-羟色胺3型受体激动剂。 AM9405抑制回肠和结肠的抽搐收缩，IC50分别为45.71 和 0.076 nM。AM9405 在生理条件下显着减缓小鼠肠道蠕动. |
|
T37206
|
CCK (27-33) (non-sulfated)
|
|
|
|
CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in m... |
|
T70267
|
ADL 08-0011 HCl
|
Others |
Others |
|
ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverse... |
|
T37996
|
17-phenyl trinor Prostaglandin E2 ethyl amide
17-phenyl trinor Prostaglandin E2 ethyl amide
|
Others |
Others |
|
17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to inc... |
|
T73930
|
(-)-Eseroline fumarate
|
Others |
Others |
|
(-)-Eseroline fumarate 是一种 AChE 抑制剂 Physostigmine 的代谢产物。(-)-Eseroline fumarate 引起癌细胞的乳酸脱氢酶 (LDH) 泄漏。(-)-Eseroline fumarate 还诱导神经元细胞释放腺嘌呤核苷酸和5-羟色胺 (5-HT)，从而诱导细胞死亡。(-)-Eseroline fumarate 抑制小鼠输精管和豚鼠回肠的电诱发抽搐。 |
|
T75868
|
JMV 449 acetate
|
Others |
Others |
|
JMV 449 acetate 是一种有效的神经降压素受体 (neurotensin receptor) 激动剂。JMV 449 acetate 显示抑制125I-neurotensin 与新生小鼠脑结合的 IC50为 0.15 nM，对收缩豚鼠回肠的 EC50为 1.9 nM。JMV 449 acetate 对小鼠具有高效、持久的降温和缓解疼痛作用。 |
|
T39176
|
PB28
|
Others |
Others |
|
PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the abi... |
|
T84522
|
14,15-Leukotriene C4
Eoxin C4
|
Others |
Others |
|
Leukotriene C4 (14,15-LTC4) is an inflammatory mediator synthesized from arachidonic acid through the actions of 15- and 12-lipoxygenases (LOs), involving intermediates such as 15-HpETE and 14,15-LTA4. Unlike the majority of leukotrienes formed via the 5-LO pathway, 14,15-LTC4 is an eoxin predominantly produced by eosinophils, although mast cells and nasal polyps can also synthesize it. While its physiological roles are not well understood, 14,15-LTC4 exhibits limited contractile activity on gui... |
|
T37261
|
14,15-Leukotriene D4
14,15-Leukotriene D4
|
Others |
Others |
|
14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both ... |
|
T68219
|
Peraclopone
|
Others |
Others |
|
Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which... |
|
T85180
|
GGTI 2133 TFA
|
Others |
Others |
|
GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. ... |
|
T36554
|
TMB 8 (hydrochloride)
|
Others |
Others |
|
TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671/RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration o... |
|
T70456
|
Nolpitantium Free Base
|
Others |
Others |
|
Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no eff... |
|
T36660
|
Olsalazine-13C6
Olsalazine-13C6
|
Others |
Others |
|
Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of ... |
|
T10165
|
5-A-RU
5-Amino-6-(D-ribitylamino)uracil
|
Others |
Others |
|
5-A-RU (5-Amino-6-(D-ribitylamino)uracil), a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules that are derived fromBencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO... |
|
T12738
|
Rivanicline hemioxalate
RJR-2403 hemioxalate,(E)-Metanicotine hemioxalate
|
Others |
Others |
|
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) 是一种神经元烟碱受体 (neuronal nicotinic receptor) 激动剂，对 α4β2 亚型有高度选择性(Ki= 26 nM)，比对于 α7 受体的选择性高1000倍(Ki=3.6 μM)。 |
|
T83768
|
Zofenoprilat
Zofenopril-SH,SQ 26,333
|
Others |
Others |
|
Zofenoprilat是一种血管紧张素转换酶(ACE; IC50 = 8 nM for the rabbit lung enzyme)的抑制剂，同时也是前体药zofenopril的活性代谢产物。它能够抑制分离的豚鼠小肠中由血管紧张素I或缓激肽诱导的收缩(EC50s = 3 and 1 nM, respectively)。在人类脐静脉内皮细胞(HUVECs)中，Zofenoprilat (10 nM)降低基础内皮素-1分泌和一氧化氮(NO)生成，并阻止TNF-α诱导的活性氧种(ROS)增加以及谷胱甘肽(GSH)水平降低。Zofenoprilat (10 µM)保护初级人类心脏微血管内皮细胞免受多柔比星诱导的细胞毒性。此外，Zofenoprilat (10 µM)还能增加HUVECs中的硫化氢(H2S)生成，以及细胞的黏着、迁移和增殖。在以400 µM浓度使用时，它可以减少Langendorff分离的大鼠心脏灌流缺血再灌注损伤模型中的舒张末压和乳酸脱氢酶(LDH)释放。 |
|
T36618
|
Rupatadine
|
Others |
Others |
|
Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu... |
|
T63399
|
mTOR/HDAC-IN-1
|
Others |
Others |
|
mTOR/HDAC-IN-1 (Compound 50) 是一个具有选择性的mTOR 和HDAC 双重抑制剂，对mTOR 和HDAC1的IC50分别为0.49和0.91 nM。 mTOR/HDAC-IN-1 可作为抗癌活性分子 （anti-cancer） 进行研究。该化合物的粉末形式不稳定，建议选择其他盐形式产品。 |
沪公网安备 31010602006700号