CID-1067700|314042-01-8|(ML282)-陌孚医药/Medlife

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CID-1067700 (Synonyms: ML282)

目录号: PL10891 纯度: ≥98%

CAS No. :314042-01-8

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中文名称	CID-1067700
中文别名	2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氢-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸;2-(3-苯甲酰硫脲基)5,5-二甲基-5,7-二氢-4H-噻吩[2,3-C]吡喃-3-羧酸;2-(3-苯甲酰硫脲基)5,5-二甲基-5,7-二氢-4H-噻吩[2,3-C]吡喃-3-甲酸;化合物CID-1067700;2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氢-5,5-二甲基-5H-噻吩并[2,3-c]吡喃-3-羧酸
英文名称	CID-1067700
英文别名	CID-1067700;2-(Benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic Acid;2-(3-Benzoylthioureido)-5,5-dimethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxylic acid;2-[[(Benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-5H-thieno[2,3-c]pyran-3-carboxylic acid;CID1067700;CID-1067700,2-(3-benzoylthioureido)-5,5-diMethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxylic acid;SID57578339;CS-1986;5H-Thieno[2,3-c]pyran-3-carboxylic acid, 2-[[(benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-;ML282,competitively,CID1067700,brain,Rab7,ML 282,GTPase,Ras,machinery,Ras-related,CID-1067700,ML-282,inhibit,CSR,Inhibitor,CID 1067700;2-(Benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acid
Cas No.	314042-01-8
分子式	C₁₈H₁₈N₂O₄S₂
分子量	390.48
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	CID-1067700 (ML282) 是 pan GTPase 抑制剂，可竞争性抑制大脑 7 (Rab7) 中的 Ras 相关蛋白，K_i 为 13 nM。
生物活性	CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a K i of 13 nM.
性状	Solid
IC50 & Target[1][2]	Ki: 13 nM (Rab7)
体外研究(In Vitro)	CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Rab7 with a Ki of 13 nM. CID-1067700 shows inhibitory activity against nucleotide binding by Rab7, with Kds of 100 nM and 40 nM for BODIPY-GTP and BODIPY-GDP, respectively. With increasing concentration, CID-1067700 causes strong inhibition on binding of the BODIPY-linked nucleotides, with EC50 values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated Ki values of 12.89 nM and 19.70 nM respectively. CID-1067700 (10 μM) has no effect on the rate of release of bound BODIPY-linked nucleotide by wild type Rab7 under equilibrium binding conditions. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells. Furthermore, CID-1067700 binds Rab7 with a high affinity (EC50: 10-20 nM), an
体内研究(In Vivo)	CID-1067700 (ML282; 16 mg/kg, i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/Fas mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo. 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]. Agola JO, et al. A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition. ACS Chem Biol. 2012 Jun 15;7(6):1095-108. [2]. Lam T, et al. Small Molecule Inhibition of Rab7 Impairs B Cell Class Switching and Plasma Cell Survival To Dampen the Autoantibody Response in Murine Lupus. J Immunol. 2016 Nov 15;197(10):3792-3805.

溶解度数据	In Vitro: DMSO : 12.5 mg/mL (32.01 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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