GPCR/G protein(G 蛋白偶联受体/G 蛋白)

Cat.No. 产品名称 Information

GC33654 MRS1186 MRS1186是人类腺苷A3受体(hA3AR)有效的、选择性拮抗剂，其Ki值为7.66nM。

GC33652 MRS1177 MRS1177是人类腺苷A3受体(hA3AR)有效的、选择性拮抗剂，其Ki值为0.3nM。

GC33559 Netupitant metabolite Monohydroxy Netupitant (Monohydroxy Netupitant)

奈妥匹坦杂质A,Monohydroxy Netupitant

Monohydroxy Netupitant 是 Netupitant 的代谢物，Netupitant 是一种高选择性的 NK1 受体拮抗剂。

GC33550 LCB-2853 LCB-2853是thromboxaneA2受体的拮抗剂，具有抗血小板和抗血栓的作用。

GC33540 OT-R antagonist 2 (Oxytocin receptor antagonist 2)

Oxytocin receptor antagonist 2

OT-R 拮抗剂 2（催产素受体拮抗剂 2）是一种非肽类低分子量 OT-R 拮抗剂。

GC33471 p-Hydroxycinnamic acid (NSC 59260)

对羟基肉桂酸

p-Hydroxy-cinnamic Acid has in vitro antimalarial activity and in vivo anti-osteoporotic properties.

GC33434 Methacholine chloride

醋甲胆碱; Acetyl-β-methylcholine chloride

A muscarinic receptor agonist

GC19486 LIT-927

LIT-927游离

A neutraligand of CXCL12

GC33413 USL311 USL311是一种选择性的CXCR4拮抗剂，具有抗癌作用。

GC33410 L-771688 L-771688是一个选择性α1A-Adrenoceptor受体拮抗剂，Ki值为0.43±0.02nM。

GC33344 WAY 163909

(8AR,11AR)-9H-4,5,6,7,8A,10,11,11A-八氢环戊并[4,5]吡咯并[3,2,1-JK][1,4]苯并二氮杂卓

WAY163909是有效的且有选择性的5-HT(2C)receptor激动剂,Ki值为10.5±1.1nM。

GC33340 BDP9066 BDP9066是肌强直性肌营养不良相关Cdc-42结合激酶MRCK的选择性有效抑制剂，其在SCC12细胞中测得对MRCKβ的IC50值为64nM，对MRCKα/β的Ki值分别为0.0136nM和0.0233nM。BDP9066通过降低底物磷酸化来治疗皮肤癌。

GC33186 BAY-293

(R)-6,7-二甲氧基-2-甲基-N-(1-(4-(2-((甲基氨基)甲基)苯基)噻吩-2-基)乙基)喹唑啉-4-胺

An inhibitor of the K-Ras-SOS1 protein-protein interaction

GC33167 Rhosin An inhibitor of the Rho-GEF protein-protein interaction

GC33154 DFMTI (MK5435)

MK5435

DFMTI (MK5435) 可以完全阻断 rmGlu1 L757V 谷氨酸反应。

GC33153 K-Ras-IN-1 K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.

GC33152 ML-18 A BB₃ receptor antagonist

GC33146 CFMTI CFMTI是一个强的，有选择性的mGluR拮抗剂，IC50是2.6nM.

GC32970 MBQ-167

MBQ-167是Ras相关的C3型肉毒素底物(Rac)和细胞分裂周期蛋白(Cdc42)的双抑制剂，其对Rac1/2/3的IC50值为103nM，对Cdc42的IC50值为78nM。

GC32905 Alprenolol ((RS)-Alprenolol)

阿普洛尔; (RS)-Alprenolol; dl-Alprenolol

A non-selective β-AR and 5-HT receptor antagonist

GC32821 Noscapine ((S,R)-Noscapine)

那可汀

Noscapine是一种口服止咳药,主要通过其σ受体激动剂活性调节,且Noscapine具有抗癌活性。

GC32776 Pentagastrin (ICI-50123)

五肽胃泌素; ICI-50123

A CCK₂ receptor agonist

GC32770 1A-116 1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes.

GC32749 Sincalide (CCK-8)

辛卡利特; Cholecystokinin octapeptide; CCK-8; SQ19844

辛卡利特(CCK-8)是CCK的一个次要生物活性片段，保留了CCK的大部分生物活性，被广泛用于研究CCK的功能。

GC32742 INT-767 INT-767是法尼醇X受体/TGR5双激动剂，平均EC50分别为30和630nM。

GC32734 CPI-444 (V81444)

V81444; ciforadenant

An adenosine A_2A receptor antagonist

GC32729 Rhosin hydrochloride

G04

An inhibitor of the Rho-GEF protein-protein interaction

GC32716 Pan-RAS-IN-1 Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.

GC32707 AZD-5069 A CXCR2 antagonist

GC32675 GP531 GP531是一种有效的第二代腺苷(adenosine)调节剂，在基础条件下药理学沉默，但在缺血期间增加局部内源性腺苷。

GC32674 A81988 (Abbott81988)

Abbott81988

A81988 (Abbott81988) 是一种有效的、竞争性的、非肽类血管紧张素 AT1 受体拮抗剂。

GC32670 L-765314 L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.

GC32667 Nuvenzepine

奴文西平

Nuvenzepine是mAChR的拮抗剂，之前在临床一期试验中用来治疗胃痉挛。

GC32666 Timepidium bromide (Sesden)

噻哌溴铵,Sesden; SA504

Timepidium bromide (Sesden) (Sesden; SA504) 是一种抗胆碱能药物。

GC32665 Bometolol Hydrochloride

波美洛尔盐酸盐

BometololHydrochloride是一种beta-adrenergic阻滞剂，可用于高血压等心血管疾病的研究。

GC32664 5-HT2A antagonist 1 5-HT2Aantagonist1是来自专利US5728835A和JP1007727的5-HT2A拮抗剂。5-HT2Aantagonist1可能用于治疗心血管疾病的研究。

GC32662 Guanoxabenz (Hydroxyguanabenz)

胍诺沙苄,Hydroxyguanabenz

Guanabenz (GBZ, GA, Wytensin, Wy-8678,BR-750) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.

GC32655 5-HT2 antagonist 1 5-HT2antagonist1是一种有效的5-HT2receptor拮抗剂，同时对α1adrenoceptor有微弱地抑制作用。

GC32654 Relacorilant (CORT 125134) Relacorilant (CORT125134) is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively.