Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4329 |
CP 376395
CP-316311 |
CRFR | GPCR/G Protein |
CP 376395 (CP-316311)是一种 CRF1受体选择性拮抗剂。 | |||
T12492 |
Pivagabine
CXB-722,匹伐加宾 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Pivagabine (CXB-722) 是疏水性 4-氨基丁酸的衍生物,具有神经调节活性。它可穿透大鼠的血脑屏障,拮抗足部休克对大鼠脑中 GABAA 受体功能和促肾上腺皮质激素释放因子 (CRF) 浓度的影响。 | |||
T7361 |
Verucerfont
NBI77860,3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺,GSK561679 |
CRFR | GPCR/G Protein |
Verucerfont (NBI77860) 是促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂,作用于 CRF1(IC50:6.1 nM),CRF2 (IC50>1000 nM)和 CRF-BP (IC50>1000 nM)。 | |||
TP1021 |
Urocortin, human
Urocortin (human),Human urocortin,Human urocortin 1,Human urocortin I |
CRFR | GPCR/G Protein |
Urocortin, human (Human urocortin I) 是由 40 个氨基酸组成的神经多肽,是选择性 CRF2受体激动剂,作用于 hCRF1(Ki:0.4 nM)、rCRF2α(Ki:0.3 nM)、 mCRF2β(Ki:0.5 nM)。 | |||
T31095 |
Crinecerfont
SSR125543,SSR 125543,SSR-125543,SSR125543A,SSR 125543A,SSR-125543A |
CRFR | GPCR/G Protein |
Crinecerfont (SSR-125543) 是促肾上腺皮质激素释放因子 1 受体 (CRF1) 的特异性拮抗剂,可用于经典先天性肾上腺增生的研究。 | |||
T16475 |
Pexacerfont
BMS-562086 |
CRFR | GPCR/G Protein |
Pexacerfont (BMS-562086) 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂,作用于人 CRF1 受体,IC50 为 6.1±0.6 nM。 | |||
TP1448L |
Astressin acetate
Astressin acetate (170809-51-5 Free base) |
CRFR | GPCR/G Protein |
Astressin acetate 是促肾上腺皮质激素释放因子 (CRF) 的拮抗剂,对 CRF 结合蛋白具有低亲和力,对克隆垂体受体具有高亲和力 (Ki = 2 nM)。 | |||
T12276 |
NVS-CRF38
|
Others | Others |
NVS-CRF38 is an antagonist of corticotropin-releasing factor receptor 1 (CRF1). | |||
T27227 |
E2508
E 2508,E-2508 |
||
E2508 is a selective antagonist of corticotropin-releasing factor 1 receptor. | |||
T15214 |
Emicerfont
GW876008 |
Others | Others |
Emicerfont is an antagonist of the corticotropin-releasing factor type 1 receptor (IC50: 66 nM). | |||
T26856 |
BMS-764459
|
||
BMS-764459 is a potent antagonist of corticotropin-releasing factor/hormone receptor 1 (CRHR-1). | |||
T23067 |
NGD 98-2 hydrochloride
|
Others | Others |
corticotropin-releasing factor receptor 1 (CRF1) antagonist | |||
T25864 |
NGD9002
NGD-9002,NGD 9002 |
||
NGD9002 is a novel generation, topology 2 selective corticotropin releasing factor-1 (CRF-1) receptor antagonist agent. | |||
T71294 | BMS-763534 | ||
BMS-763534 is a potent antagonist of corticotropin-releasing factor/hormone receptor 1 (CRHR-1). | |||
T69248 |
ONO-2333
|
||
ONO-2333 is a corticotropin-releasing factor receptor antagonist, for the treatment of depression and/or anxiety disorders | |||
T69374 |
NGD 98-2
|
||
NGD 98-2 is a new generation, topology 2 selective orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist. | |||
T38228 |
R 121919 hydrochloride
|
||
High affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable. Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216 |Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919... | |||
TP1860 |
Urocortin II, human
|
||
Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor. | |||
TP2048 |
α-Helical CRF(9-41)
α-helical CRF 9-41 |
||
Corticotropin-releasing factor receptor antagonist (Ki values are 17, 5 and 0.97 at human CRF1, rat CRF2α and mouse CRF2β receptors respectively). | |||
TP2095 |
Astressin 2B
|
||
Potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist (IC50 values are 1.3 and > 500 nM for CRF2 and CRF1 respectively). Antagonizes CRF2-mediated inhibition of gastric emptying. | |||
TP2121 |
Sauvagine
|
||
Corticotropin-releasing factor (CRF) receptor agonist. Ki values are 9.4, 9.9, and 3.8 nM for inhibition of 125I-[D-Tyr1]astressin binding to hCRF-R1, rCRF-R2a and mCRF-R2b respectively. | |||
TP2125 |
Stressin I
|
||
Potent and selective corticotropin releasing factor receptor-1 (CRF1) agonist (Ki values are 1.5 and 224 nM for CRF1 and CRF2 receptors respectively). Increases ACTH levels and increases faecal pellet output in vivo following i.p. administration. | |||
T26855 |
BMS-665053
BMS665053 |
||
BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addi | |||
TP2091 |
Antisauvagine-30
|
||
Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells | |||
TP1557 |
Urocortin II, human TFA
|
||
Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor. Human urocortin II exhibits mild motor-suppressive effects and delayed anxiolytic-like effects,suggesting a time-depen | |||
T76492 |
(Tyr0)-Urocortin, rat
|
||
(Tyr0)-Urocortin, rat 是针对促肾上腺皮质激素释放因子受体1型(CRF-R1)和2型(CRF-R2)的高亲和力激动剂,其抑制结合常数(Ki)为1-2 nM。 | |||
T35814 |
Urocortin III (human) (trifluoroacetate salt)
|
||
Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively).... | |||
T76127 |
Urocortin II, mouse
|
||
Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂,对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP/PKA 和 Ca2+/CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达,并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。 | |||
T76180 |
Urocortin III (human)
|
||
Urocortin III (human) 是一种促肾上腺皮质激素释放因子 (CRF) 相关肽。Urocortin III (human) 优先结合并激活CRF-R2,并且具有离散的中枢神经系统和外周分布。Urocortin III (human) 选择性结合 2 型 CRF 受体,mCRF2β、rCRF2α 和 hCRF1 的Ki 值分别为 13.5、21.7 和 >100 nM。Urocortin III (human) 介导Insulin(human) 分泌的生长抑素依赖性负反馈控制。 | |||
T83674 |
K 41498 TFA
|
||
K 41498 是一种针对皮质酮释放因子受体2α(CRF2α)和CRF2β的肽拮抗剂,其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性,与CRF1相比(在表达人类受体的HEK293细胞中Ki值为425 nM)。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药,K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。 |