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Cat. No. | Product Name | ||
---|---|---|---|
L7110 | 抗高血压化合物库 | 678 compounds | |
678 种高血压相关的小分子,用于高通量和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP1181 |
Bradykinin (2-9)
Des-Arg1-bradykinin |
Bradykinin Receptor | GPCR/G Protein |
Bradykinin (2-9) (Des-Arg1-bradykinin),是Bradykinin的一种氨基端截短肽类代谢物,通过Aminopeptidase P的切割作用形成。 | |||
TP1277 |
Bradykinin
缓激肽 |
Endogenous Metabolite; Bradykinin Receptor | GPCR/G Protein; Metabolism |
Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。 它是炎症调节因子和神经调节因子,对几种血管和肾功能也有调节作用。 | |||
TP1445 |
[Des-Arg9]-Bradykinin acetate
[Des-Arg9]-缓激肽醋酸盐 |
Bradykinin Receptor | GPCR/G Protein |
[Des-Arg9]-Bradykinin acetate 是一种选择性缓激肽 B1 受体激动剂。 | |||
T5048 |
SSR240612
|
Bradykinin Receptor | GPCR/G Protein |
SSR240612 是口服有活性的非肽类缓激肽 B1 (bradykinin B1) 受体特异性拮抗剂。 | |||
T22344 |
Icatibant Acetate
|
Bradykinin Receptor | GPCR/G Protein |
Icatibant acetate 是一种特异性缓激肽 B2 受体拮抗剂,其 IC50=1.07 nM,Ki=0.798 nM。 | |||
T2086 |
ELN-441958
ELN 441958 |
Bradykinin Receptor | GPCR/G Protein |
ELN-441958是一种B1受体拮抗剂,能够抑制B1激动剂配体[3H] DAKD 与IMR-90细胞结合(Ki:0.26 nM),相较于B2受体,它对B1受体的抑制作用具有更高的选择性,且比抑制μ阿片受体选择性高500多倍,比抑制δ阿片受体选择性高2000多倍。 | |||
T7645 |
[Des-Arg9]-Bradykinin
[Des-Arg9]-Bradykinin(2TFA),[Des-Arg9]-缓激肽 |
Bradykinin Receptor | GPCR/G Protein |
[Des-Arg9]-Bradykinin ([Des-Arg9]-Bradykinin(2TFA)) 是 Bradykinin(B1) 受体激动剂,对 B1受体选择性大于B2受体。 | |||
T8809 |
[Des-Arg9]-Bradykinin TFA
|
Bradykinin Receptor | GPCR/G Protein |
[Des-Arg9]-Bradykinin TFA 是一种缓激肽 (B1) 受体激动剂,对 B1 的选择性优于对 B2 受体的选择性。 | |||
T36442L |
(Hyp³)-Bradykinin acetate
(Hyp³)-Bradykinin acetate (37642-65-2 Free base) |
Bradykinin Receptor | GPCR/G Protein |
(Hyp³)-Bradykinin acetate 是一种缓激肽 B2 受体激动剂,可刺激培养的人成纤维细胞中磷酸肌醇的产生。 | |||
TP2268L |
Lys-Bradykinin acetate(342-10-9 free base)
|
Bradykinin Receptor | GPCR/G Protein |
Lys-Bradykinin acetate(342-10-9 free base) 是一种内源性缓激肽受体激动剂。 | |||
T33421 |
MK-0686
MK0686 |
Bradykinin Receptor | GPCR/G Protein |
MK-0686 是一种可口服的缓激肽 B1 受体拮抗剂,具有潜在的抗炎活性。 | |||
TP2075L |
Bombinakinin M acetate
Bombinakinin M acetate(509151-65-9 free base) |
Bradykinin Receptor | GPCR/G Protein |
Bombinakinin M acetate 是一种有效的缓激肽受体激动剂,对哺乳动物动脉平滑肌缓激肽受体具有高度选择性,其效力比缓激肽高约 50 倍。 | |||
TP1918L |
Lys-[Des-Arg9]Bradykinin,TFA
Lys-[Des-Arg9]Bradykinin,TFA 71800-36-7(fb-tfa) |
Bradykinin Receptor | GPCR/G Protein |
Lys-[Des-Arg9]Bradykinin,TFA (71800-36-7 free base) 是内源性强效和高选择性的缓激肽 B1 受体激动剂(对人 B1 和 B2 受体的 Ki 值分别为 0.12 和 > 30000 nM)。降低体内外周血管阻力的降压药。比 [Des-Arg9]-缓激肽强 16 倍。 | |||
TP1918L1 |
Lys-[Des-Arg9]Bradykinin acetate
Lys-[Des-Arg9]Bradykinin acetate (71800-36-7 free base) |
Bradykinin Receptor | GPCR/G Protein |
Lys-[Des-Arg9]Bradykinin acetate (71800-36-7 free base) 是一种内源性强效和高选择性的缓激肽 B1 受体激动剂(对人 B1 和 B2 受体的 Ki 值分别为 0.12 和 > 30000 nM)。降低体内外周血管阻力的降压药。比 [Des-Arg9]-缓激肽强 16 倍。 | |||
T34485 |
Safotibant
LF220542,LF 220542,LF 22-0542,LF-220542,LF-22-0542,LF22-0542 |
Bradykinin Receptor | GPCR/G Protein |
Safotibant (LF-22-0542) 是一种缓激肽 B1 受体拮抗剂,具有抗炎和镇痛活性,可用于局部治疗糖尿病性黄斑水肿。 | |||
TP1917L1 |
Sar-[D-Phe8]-des-Arg9-Bradykinin acetate
Sar-[D-Phe8]-des-Arg9-Bradykinin acetate(126959-88-4 free base) |
Bradykinin Receptor | GPCR/G Protein |
Sar-[D-Phe8]-des-Arg9-Bradykinin acetate(126959-88-4 free base) 是一种有效的选择性缓激肽 B1 受体激动剂(兔主动脉中的 EC50 = 9.02 nM),对氨肽酶、激肽酶 I 和 II (ACE) 以及中性内肽酶切割具有抗性。在体内表现出降血压和血管生成活性。 | |||
T26627L |
Anatibant 2HCl
Anatibant 2HCl(209733-45-9 Free base) |
Bradykinin Receptor | GPCR/G Protein |
Anatibant 2HCl 是一种小分子缓激肽B2受体拮抗剂,可用于治疗神经系统疾病,可能用于研究脑损伤。 | |||
TP1933 |
R715 TFA(185052-09-9 free base)
R 715 |
Bradykinin Receptor | GPCR/G Protein |
R715 TFA(185052-09-9 free base) 是强效和选择性缓激肽 B1 受体拮抗剂 (pA2 = 8.49)。它对B2 受体无活性。它减少神经性疼痛小鼠模型中的机械性过度伤害感受。它代谢稳定。 | |||
TP1931L1 |
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate(96736-12-8 free base) |
cholecystokinin | GPCR/G Protein |
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate ([D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate (96736-12-8 free base)) 是广谱神经肽反向激动剂和拮抗剂。 ghrelin 受体的强效完全反向激动剂(EC50 = 5.2 nM);减少组成型生长素释放肽受体信号传导。它也是速激肽、缓激肽、CCK 和铃蟾肽受体的拮抗剂。在体外诱导细胞凋亡并抑制癌细胞生长。 | |||
T4200 |
Sacubitril hemicalcium salt
AHU-377 (hemicalcium salt),LCZ696中间体,AHU377 calcium salt |
Neprilysin | Metabolism |
Sacubitril hemicalcium salt (AHU377 calcium salt) 是一种有效的 NEP 抑制剂,IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。 | |||
T15347 | FR167344 free base | Others | Others |
FR167344 free base is an orally active and nonpeptide antagonist of bradykinin receptor B2. FR167344 free base displays a high-affinity binding to the B2 receptor (IC50: 65 nM). It has no binding affinity for the B1 receptor. | |||
T25555 |
JMV-1645
JMV1645,JMV 1645 |
Others | Others |
JMV-1645 is an effective and selective B(1) bradykinin receptor antagonist. | |||
T24065 |
FK-3657
FK 3657,FK3657,FR-173657,FR 173657,FR173657 |
Others | Others |
FK-3657 is a non-peptide antagonist of bradykinin (BK)-B2 receptor. | |||
T27377 |
FR190997
FR-190997,FR 190997 |
Others | Others |
FR190997 is an agonist of bradykinin B2 receptor. | |||
T21060 |
NPC 567
|
||
NPC 567 is an antagonist of the bradykinin receptor. | |||
T70576 |
NPC 17731
|
Others | Others |
NPC 17731 is a bradykinin receptor antagonist. | |||
T70574 |
NPC 17761
|
Others | Others |
NPC 17761 is a bradykinin receptor antagonist. | |||
T63241 |
Fulimetibant
|
Others | Others |
Fulimetibant 是缓激肽受体 (bradykinin receptor) 拮抗剂。 | |||
T25895 |
NVP-SAA164
SAA 164,SAA164,SAA-164,NVP SAA164 |
Others | Others |
NVP-SAA164 is a nonpeptide bradykinin B1 receptor antagonist agent. | |||
T70750 |
Deltibant
|
Others | Others |
Deltibantis a bradykinin receptor antagonist. | |||
TP2268 |
Lys-Bradykinin
|
Others | Others |
Endogenous bradykinin receptor agonist | |||
T76385 |
[Tyr8] Bradykinin
|
||
[Tyr8] Bradykinin 是B2激肽受体 (B2kinin receptor) 的激动剂,能刺激ERK1/2磷酸化,并可作为内标。 | |||
T80117 |
Lys-(Des-Arg9,Leu8)-Bradykinin
|
Bradykinin Receptor | GPCR/G Protein |
Lys-(Des-Arg9,Leu8)-Bradykinin为缓激肽B1受体的拮抗剂。 | |||
T80072 |
Des-Arg9-[Leu8]-Bradykinin acetate
|
Bradykinin Receptor | GPCR/G Protein |
Des-Arg9-[Leu8]-Bradykinin acetate 是一种B1R(缓激肽受体1)拮抗剂,主要应用于肾纤维化的研究。 | |||
T76212 |
B 9430
|
||
B 9430 是一种有效的缓激肽 B1/B2 受体拮抗剂。 | |||
T83500 |
[Des-Arg10]-HOE I40
|
||
[Des-Arg10]-HOE 140 是一种有效的 B1 缓激肽受体拮抗剂,具备生物活性。 | |||
TP2076 |
[Phe8Ψ(CH-NH)-Arg9]-Bradykinin
|
||
Selective bradykinin B2 receptor agonist that is resistant to carboxypeptidase cleavage. 5-fold more potent and exhibits a more prolonged duration of action than bradykinin in vivo. | |||
T38544 |
Fasitibant chloride
MEN16132 free base,Fasitibant chloride |
Others | Others |
Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis. | |||
T15547 |
Icatibant
艾替班特,HOE 140 |
Others | Others |
Icatibant is a selective and specific antagonist of the bradykinin B2 receptor (IC50 and Ki: 1.07 nM and 0.798 nM respectively). | |||
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 | |||
TP1931 |
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
|
||
Broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. In | |||
T27790 |
Labradimil
RMP-7,ALK-01-040,Receptor-mediated permeabiliser-7,DRG0182,DRG 0182,DRG-0182 |
||
Labradimil is a bradykinin B2 receptor agonist. Labradimil increases the permeability of human brain microvascular endothelial cell monolayers. Labradimil enhances delivery of hydrophilic chemotherapeutics and increases survival in rats with metastatic tu | |||
TP1918 |
Lys-[Des-Arg9]Bradykinin
|
||
Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9] | |||
T26627 |
Anatibant
LF16-0687,LF-16-0687,LF 160687,LF 16-0687,LF-160687 |
Others | Others |
Anatibant 是一种有效的非肽缓激肽B2受体拮抗剂。Anatibant 降低实验性外伤性脑损伤后颅内高压和组织病理学损伤。 | |||
T73646 |
Lys-[Des-Arg9]Bradykinin TFA
|
||
Lys-[Des-Arg9]Bradykinin TFA 是一种天然存在的激肽,是一种有效且高度选择性的缓激肽 B1受体激动剂,对人,小鼠和兔子的 B1受体的 Ki 值为 0.12 nM,1.7 nM 和 0.23 nM。Lys-[Des-Arg9]Bradykinin TFA 对 B2 受体的抑制活性较低。 | |||
TP1917 |
Sar-[D-Phe8]-des-Arg9-Bradykinin
|
||
Potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo. | |||
TP1999 |
MEN 11270
|
||
Peptide antagonist of the B2 bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140. Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5). | |||
TP1662 |
Galanin Receptor Ligand M35
|
||
The chimeric peptide M35 [galanin (1-13)-bradykinin(2-9) amide] is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. The radiolabelled M35 and perf | |||
TP2126 |
R 892
|
||
Potent and selective bradykinin B1 receptor antagonist (ID50 values are 2.8 and > 600 nM at B1 and B2 receptors respectively). Exhibits no intrinsic agonist activity and is resistant to aminopeptidase and kininase II (ACE) cleavage. Displays hypertensive | |||
T83688 |
R 715 TFA
[Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH |
||
R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩(pA2 = 8.49)。R 715(200、400及600 µg/kg)通过尾部闪烁测试减少了由链脲佐菌素(STZ)诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白(MOG)(35-55)(MOG35-55)抗原肽诱导的实验性自体免疫性脑炎(EAE)小鼠模型中,通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率,改善对称步态,并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715(0.01 nmol/动物,脑室内)能在自发性高血压大鼠中降低平均动脉血压并增加心率。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-00410 |
EPHX2 Protein, Human, Recombinant (His)
SEH,CEH,epoxide hydrolase 2, cytoplasmic |
Human | Baculovirus Insect Cells |
Genetic variation in EPHX2 was significantly associated with risk of incident CHD in Caucasians, implicating EPHX2 as a potential cardiovascular disease-susceptibility gene. Single nucleotide polymorphisms (SNPs) in the human EPHX2 gene had been implicated in susceptibility to cardiovascular disease, including stroke. The human EPHX2 mutations may in part explain the genetic variability in sensitivity to ischemic brain injury and stroke outcome. Epoxide hydrolase is involved in metabolism of vas... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T69673 |
Deucrictibant
|
||
Deucrictibant is a bradykinin receptor antagonist. |