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GRK2 Inhibitor_24269-96-3_产品详情
24269-96-3
  • 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
GRK2 Inhibitor
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中文别名 GRK2 Inhibitor
英文别名 GRK2 Inhibitor; βARK1 Inhibitor;
CAS号 24269-96-3
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
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。
IntroductionGRK2 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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