24269-96-3|GRK2 Inhibitor|5-[2-(5-Nitro-furan-2-yl)-vinyl]-furan-2-carboxylic acid methyl ester|-范德生物科技公司

GRK2 Inhibitor

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names：
5-[2-(5-Nitro-furan-2-yl)-vinyl]-furan-2-carboxylic acid methyl ester
CAS号：
24269-96-3
MDL Number：
MF(分子式)： C12H9NO6 MW(分子量)： 263.2
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	GRK2 Inhibitor
英文别名	GRK2 Inhibitor; βARK1 Inhibitor;
CAS号	24269-96-3
SMILES	O=C(C1=CC=C(/C=C/C2=CC=C([N+]([O-])=O)O2)O1)OC
Inchi	InChI=1S/C12H9NO6/c1-17-12(14)10-6-4-8(18-10)2-3-9-5-7-11(19-9)13(15)16/h2-7H,1H3/b3-2+
InchiKey	YDJPHSNZGRVPCK-NSCUHMNNSA-N
分子式 Formula	C12H9NO6
分子量 Molecular Weight	263.2
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	GRK2 Inhibitor(CAS:24269-96-3):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	GRK2 Inhibitor is an inhibitor of GRK 2 (β-Adrenergic Receptor Kinase 1).
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Wang HJ, Gu HX, Eijkelkamp N, Heijnen CJ, Kavelaars A. Low GRK2 Underlies Hyperalgesic Priming by Glial Cell-Derived Neurotrophic Factor. Front Pharmacol. 2018 Jun 5;9:592. doi: 10.3389/fphar.2018.00592. eCollection 2018. PubMed PMID: 29922165; PubMed Central PMCID: PMC5996251.

[2]Crassini K, Pyke T, Shen Y, Stevenson WS, Christopherson RI, Mulligan SP, Best OG. Inhibition of the Raf-1 kinase inhibitory protein (RKIP) by locostatin induces cell death and reduces the CXCR4-mediated migration of chronic lymphocytic leukemia cells. Leuk Lymphoma. 2018 Jun 18:1-12. doi: 10.1080/10428194.2018.1455974. [Epub ahead of print] PubMed PMID: 29911936.

[3] Yu Q, Gratzke C, Wang Y, Herlemann A, Strittmatter F, Rutz B, Stief CG, Hennenberg M. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101. Eur J Pharmacol. 2018 Jul 15;831:9-19. doi: 10.1016/j.ejphar.2018.04.022. Epub 2018 Apr 23. PubMed PMID: 29698717.

[4] Im YN, Lee YD, Park JS, Kim HK, Im SY, Song HR, Lee HK, Han MK. GPCR Kinase (GRK)-2 Is a Key Negative Regulator of Itch: l-Glutamine Attenuates Itch via a Rapid Induction of GRK2 in an ERK-Dependent Way. J Invest Dermatol. 2018 Mar 9. pii: S0022-202X(18)30220-3. doi: 10.1016/j.jid.2018.02.036. [Epub ahead of print] PubMed PMID: 29530536.

[5] Kawakami M, Hattori M, Ohashi W, Fujimori T, Hattori K, Takebe M, Tomita K, Yokoo H, Matsuda N, Yamazaki M, Hattori Y. Role of G protein-coupled receptor kinase 2 in oxidative and nitrosative stress-related neurohistopathological changes in a mouse model of sepsis-associated encephalopathy. J Neurochem. 2018 Mar 3. doi: 10.1111/jnc.14329. [Epub ahead of print] PubMed PMID: 29500815.

6: Taguchi K, Bessho N, Hasegawa M, Narimatsu H, Matsumoto T, Kobayashi T. Co-treatment with clonidine and a GRK2 inhibitor prevented rebound hypertension and endothelial dysfunction after withdrawal in diabetes. Hypertens Res. 2018 Apr;41(4):263-274. doi: 10.1038/s41440-018-0016-6. Epub 2018 Feb 20. PubMed PMID: 29463871.7: Qi X, Guo Y, Song Y, Yu C, Zhao L, Fang L, Kong D, Zhao J, Gao L. Follicle-stimulating hormone enhances hepatic gluconeogenesis by GRK2-mediated AMPK hyperphosphorylation at Ser485 in mice. Diabetologia. 2018 May;61(5):1180-1192. doi: 10.1007/s00125-018-4562-x. Epub 2018 Feb 13. PubMed PMID: 29442133.8: Pusapati GV, Kong JH, Patel BB, Gouti M, Sagner A, Sircar R, Luchetti G, Ingham PW, Briscoe J, Rohatgi R. G protein-coupled receptors control the sensitivity of cells to the morphogen Sonic Hedgehog. Sci Signal. 2018 Feb 6;11(516). pii: eaao5749. doi: 10.1126/scisignal.aao5749. PubMed PMID: 29438014; PubMed Central PMCID: PMC5828112.9: Bouley R, Waldschmidt HV, Cato MC, Cannavo A, Song J, Cheung JY, Yao XQ, Koch WJ, Larsen SD, Tesmer JJG. Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol Pharmacol. 2017 Dec;92(6):707-717. doi: 10.1124/mol.117.110130. Epub 2017 Oct 25. PubMed PMID: 29070696; PubMed Central PMCID: PMC5691592.10: Zhang QH, Hao JW, Li GL, Ji XJ, Yao XD, Dong N, Yao YM. Proinflammatory switch from Gαs to Gαi signaling by Glucagon-like peptide-1 receptor in murine splenic monocyte following burn injury. Inflamm Res. 2018 Feb;67(2):157-168. doi: 10.1007/s00011-017-1104-9. Epub 2017 Oct 11. PubMed PMID: 29022064.1

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