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Cat. No. | Product Name | Target | Signaling Pathways |
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T82252 |
GTPγS tetralithium
Guanosine 5'-[γ-thio]triphosphate tetralithium |
Others | Others |
GTPγS tetralithium (Guanosine 5'-[γ-thio]triphosphate tetralithium) 是一种 G 蛋白激活剂,是一种不可水解 GTP 类似物,可保护蛋白质免遭蛋白水解降解。GTPγS tetralithium 参与检测表达重组受体的细胞以及表达内源性受体的细胞和组织中GPCR信号传导,可测定用于测量激动剂诱导的两种人多态性 α2B-肾上腺素受体变体的脱敏。 | |||
T38782 |
Mant-GTPγS
|
Others | Others |
Mant-GTPγS, an effective GTP analog, displays strong competitive inhibition of adenylyl cyclase (AC). Additionally, it acts as a potent inhibitor of YdeH. | |||
T10639 |
C-021 dihydrochloride
|
CCR | Immunology/Inflammation; Microbiology/Virology |
C-021 dihydrochloride 是一种有效的 CCR4 拮抗剂。 它有效抑制人和小鼠的功能趋化性,IC50 为 140 nM 和 39 nM。 | |||
T21870 |
C-021
4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy- |
CCR | Immunology/Inflammation; Microbiology/Virology |
C 021 dihydrochloride 是一种 CC 趋化因子受体 4 (CCR4) 拮抗剂,抑制人和小鼠的功能趋化性,IC50分别为 140 和 39 nM。C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) 可有效阻止人 CCL22 衍生的 [35S]GTPγS 与受体结合,IC50为 18 nM。 | |||
T2036 |
6-OAU
GTPL5846 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
6-OAU (GTPL5846) 是 GPR84 的替代激动剂,在 Gqi5 嵌合体存在的情况下,在 HEK293 细胞中激活人 GPR84,在 PI 测定中 EC50 为 105 nM。 | |||
T4407 |
SR17018
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
SR17018 是一种 μ-阿片受体 (MOR) 激动剂,与 GTPγS 结合,EC50 为 97 nM。 | |||
TQ0108 |
MK-6892
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
MK-6892 是烟酸受体GPR109A 选择性激动剂。它作用于人 GPR109A 的Ki=4 nM,EC50=16 nM。 | |||
T7316 |
LY2828360
|
Cannabinoid Receptor | GPCR/G Protein |
LY2828360 是一种作用缓慢的、有效的 G 蛋白偏倚的大麻素受体 2(CB2)激动剂,能够抑制 cAMP 的积累并激活 ERK1/2 通路。 | |||
T37075 |
CB2R PAM
Ec2la |
Cannabinoid Receptor | GPCR/G Protein |
CB2R PAM 是一种口服活性大麻素 2 型受体(CB2Rs)阳性突变调节剂,它能增强 CP 55940 和 2-Arachidonylglycerol 刺激的 [35S]GTPγS 与 CB2 受体的结合,但在没有激动剂的情况下没有作用。CB2R PAM 在神经病理性疼痛小鼠模型中显示出抗损伤活性。 | |||
T37610 |
AT-121
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
AT-121 是一种双重μ-阿片和神经肽受体部分激动剂(Kis 分别为 16.49 和 3.67 nM)。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合(EC50s 分别为 19.6 和 34.7 nM)。AT-121(0.003-0.03 mg/kg)能以剂量依赖的方式降低辣椒素诱导的热异感,但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中,AT-121 每次注射剂量为 0.3 至 10 μg/kg,它缺乏强化作用(一种潜在的滥用标志),不能减少食物颗粒的强化作用。AT-121(0.01 或 0.03 毫克/千克)不会诱发恒河猴的超痛觉,超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药,具有抗伤害和止痛作用。 | |||
T41231 |
GP 1a
|
Cannabinoid Receptor; PERK; Arrestin | Apoptosis; GPCR/G Protein |
GP 1a 是cannabinoid receptor 2(CB2)的强效激动剂(EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍,且在体外增加HL-60细胞的P-ERK1/2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成,同时促进上皮的重新形成。 | |||
T21935L |
AMN082 free base
AMN082 |
GluR | Neuroscience |
AMN082 free base 是 mGluR7选择性激动剂,口服有活性,能够透过血脑屏障,可通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上,它能够有效抑制 cAMP 积累并刺激 GTPγS 结合。它能够选择性针对 mGluR 的其他亚型及选择性离子型谷氨酸受体。具有抗抑郁活性。 | |||
T26869 |
BMS-986122
BMS 986122 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
BMS-986122 (BMS 986122) 是选择性 μ 阿片受体正变构调节剂,可增加 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的作用,还增强 DAMGO 介导的 [35S]GTPγS 在小鼠脑膜中的结合。 | |||
T6923 |
Ozanimod
奥扎莫德,RPC-1063 |
S1P Receptor; LPL Receptor | GPCR/G Protein |
Ozanimod (RPC-1063) 是一种选择性S1P1和S1P5受体激动剂,在[35S]-GTPγS 结合实验中,EC50分别为 410 pM 和 11 nM。它可研究治疗克罗恩病、溃疡性结肠炎、多发性硬化症和复发性多发性硬化症的试验。 | |||
T32341 |
JWH-251
|
Others | Others |
JWH 251, a cannabimimetic indole, has a high affinity tothe central cannabinoid (CB1) receptor (Ki = 29 nM) and a comparatively modest affinity for the peripheral cannabinoid (CB2) receptor (Ki = 146 nM). JWH 251 can stimulates GTPγS and bind to CB1 and | |||
T67760 |
JNJ-65355394
|
Others | Others |
JNJ-65355394 是一种有效的 O-GlcNAc 水解酶 (OGA) 抑制剂,是一种 OGA 化学探针。 | |||
T26667 |
ASN04421891
ASN 04421891,ASN-04421891 |
Others | Others |
ASN04421891 是一种 GPR17受体调节剂,在 [35S]GTPγS 结合实验中 EC50为 3.67 nM,具有神经退行性疾病的研究潜力。 | |||
T74993 |
A3AR modulator 1
|
Others | Others |
A3AR modulator 1 (MRS8054) 是口服活性 A3 腺苷受体 (A3AR(Adenosine Receptor)) 正变构调节剂 (PAM)。该化合物显著增强 Cl-IB-MECA 刺激的 [35S]GTPγS 结合 Emax。 | |||
T62918 |
GPR84 antagonist 3
|
Others | Others |
GPR84antagonist 3 (compound 42)为一种高效GPR84(G 蛋白偶联受体 84)拮抗剂,具pIC50值为8.28,表现出对GTPγS的抑制作用,并拥有良好的药代动力学特性。 | |||
T85295 |
Salvinorin A Carbamate
Divinorin A Carbamate,Sal A Carbamate |
Others | Others |
Salvinorin A carbamate, a potent κ-opioid receptor (KOR) full agonist, exhibits nearly the same potency as salvinorin A, with EC50 values of 6.2 and 4.5 nM, respectively, for activating the human KOR to augment the binding of [35S]GTPγS. Enhancing biological stability, the addition of a carbamate group to salvinorin A reduces deacetylation. | |||
T62756 |
LY487379
|
Others | Others |
LY487379是一种选择性的人类 mGluR2 阳性异生调节剂(PAM)。LY487379 可提高谷氨酸刺激的 [35 S] GTPγS 结合,作用于 mGlu2 受体 (EC50: 1.7 μM) 和 mGlu3 受体 (EC50>10 μM)。LY487379 在大鼠模型中促使认知的灵活性,并诱导行为抑制。LY487379 能够用于研究精神分裂症。 | |||
T84498 |
JWH 302
|
Others | Others |
JWH 302, a cannabimimetic indole, exhibits 5-fold selectivity for the central cannabinoid (CB1) receptor, evidenced by a Ki value of 17 nM, versus the peripheral cannabinoid (CB2) receptor, which has a Ki value of 89 nM. Additionally, JWH 302 stimulates GTPγS binding of CB1 and CB2 receptors with EC50 values of 29.3 nM and 24.4 nM, respectively. | |||
T21999 |
(±)-J 113397
|
Others | Others |
(±)-J-113397 是一种有效的、高选择性的非肽基ORL1 受体拮抗剂,对人克隆 ORL1 的Ki 为 1.8 nM。在体外,J-113397 抑制 nociceptin/orphanin FQ 刺激的GTPγS 与表达 ORL1 的 CHO 细胞结合,IC50值为 5.3 nM。J-113397 可用于研究 nociceptin/orphanin FQ 的生理作用。 | |||
T75907 |
Ac-RYYRIK-NH2 TFA
|
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Ac-RYYRIK-NH2 TFA 作为高效的ORL1部分激动剂,充当ORL1的内源性配体,在CHO细胞中表现出较低的解离常数(Kd=1.5 nM)。该化合物以特异性方式激活G蛋白,作为竞争性拮抗剂,抑制noc/OFQ对大鼠脑膜和脑切片上 [35S]-GTPγS 结合G蛋白的作用。 | |||
T84518 |
CAY10508
|
Others | Others |
CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding as... | |||
T69798 |
4-Me-PDTic HCl
|
Others | Others |
4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors, respectively. Calculated logBB and CNS (central nervous system) multiparameter optimization (MPO) and low molecular weight values all predict that 4-Me-PDTic will penetrate the brain and pharmacokinetic studies in rats shows that 4-Me-PDTic does indeed penetrate the brain. | |||
T85077 |
AKP-11
|
Others | Others |
AKP-11 is a sphingosine-1-phosphate receptor 1 (S1P1) agonist with an EC50 of 0.047 μM for [35S]GTPγS binding to CHO-K1 cell membranes expressing human S1P1. It reduces S1P1 surface expression and enhances Akt and ERK phosphorylation in CHO cells with S1P1-HA at a 100 nM concentration. At doses of 1.3 and 3 mg/kg, AKP-11 lowers IFN-γ and IL-17 protein levels in the spinal cord and mitigates disease severity in a rat experimental autoimmune encephalomyelitis (EAE) model. Additionally, it decrease... | |||
T83685 |
UFP101 TFA
|
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UFP101是一种合成肽类物质,作为nociceptin受体的拮抗剂(Ki为0.06 nM,测试于表达人类受体的CHO细胞中)。它对nociceptin受体的选择性高于κ-opioid受体(Ki为204 nM,测试于表达大鼠受体的CHO细胞中)。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS(EC50为1.86 nM)。通过脑室内给药,UFP101(10 nmol/每只动物)能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中,UFP101(0.003、0.03及0.3 mg/kg)能提高生存率。 | |||
T36722 |
Deltorphin II (trifluoroacetate salt)
|
Others | Others |
Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5081 |
Adenine monohydrochloride hemihydrate
腺嘌呤盐酸盐,Adenine hydrochloride hydrate,6-Aminopurine hydrochloride hydrate |
Endogenous Metabolite; Adenosine Receptor | GPCR/G Protein; Metabolism; Neuroscience |
Adenine monohydrochloride hemihydrate 是内源性代谢产物的一种。 | |||
T83913 |
Mitraciliatine
|
Others | Others |
Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T35591 |
Guanfacine-13C,15N3
Guanfacine-13C,15N3 |
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Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacin... |