R121919|195055-03-9|(NBI30775)-陌孚医药/Medlife

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R121919 (Synonyms: NBI30775)

目录号: PL03927 纯度: ≥99%

CAS No. :195055-03-9

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中文名称	R121919
中文别名	3-(6-(二甲基氨基)-4-甲基吡啶-3-基)-2,5-二甲基-N,N-二丙基吡唑并[1,5-A]嘧啶-7-胺
英文名称	R121919
英文别名	3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine;3-[6-(DiMethylaMino)-4-Methyl-3-pyridinyl]-2,5-diMethyl-N,N-dipropylpyrazolo[1,5-a]pyriMidin-7-aMine;3-[6-(dimethylamino)-4-methylpyridin-3-yl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine;Pyrazolo[1,5-a]pyrimidin-7-amine,3-[6-(dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-d...;Pyrazolo[1,5-a]pyrimidin-7-amine,3-[6-(dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropyl-;R-121,919;NBI30775;R 121919;UNII-G82N555U1N;-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine;3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7;3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-am;3-[6-(diMethylaMino)-4-Methyl-3-pyridinyl]-2,5-diMethyl-N,N-dipropyl-pyrazolo[2,3-a]pyriMidine-7-aMine;R121919
Cas No.	195055-03-9
分子式	C₂₂H₃₂N₆
分子量	380.53
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	R121919 (NBI30775) 是一种高效的小分子 CRF1 受体拮抗剂。对于 CRF1 受体的 K_i 值为 2 至 5 nM，对 CRF2 受体，CRF 结合蛋白或 70 种其它受体类型的活性弱超过 1000 倍。
生物活性	R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a K i of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
性状	Solid
IC50 & Target[1][2]	Ki: 2 to 5 nM (CRF1)
体外研究(In Vitro)	R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2–5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drugs intracellular targets. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80. [2]. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.

溶解度数据	In Vitro: Ethanol : 100 mg/mL (262.79 mM; Need ultrasonic)DMSO : 6.2 mg/mL (16.29 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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