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DREADD激动剂21二盐酸盐,DREADD Agonist 21 dihydrochloride;≥98% (HPLC)

别名:11-(1-piperazinyl)-5H-Dibenzo[b,e][1,4]diazepine dihydrochloride, 11-(Piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine; 11-Piperazinyldibenzo[b,e][1,4]diazepine dihydrochloride, Compound 21 dihydrochloride

CAS号 56296-18-5 (free base) 经验分子式(希尔表示法) C17H18N4 · 2HCl 分子量 351.27 MDL number MFCD25121806
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML2392
CAS号: 56296-18-5
MDL号: MFCD25121806
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$208.60

产品描述

一种毒蕈碱型HM3DQ受体激动剂,EC50:1.7 nM.

Biochem/physiol Actions

Compound 21 is a potent designer drug with full agonist activity toward human hM3Dq (EC50 = 1.7 nM by cell-based Ca2+ mobilization assay), a human M3 muscarinic receptor (M3R)-based Gq (M3Dq) DREADD (Designer Receptors Exclusively Activated by Designer Drugs), displaying little activity toward muscarinic acetylcholine receptor M3 (30% M3 activation at 10 μM) and reduced affinity toward H1, 5HT2A, 5HT2C, α1A receptor (fold selectivity = 3.5, 40, 100, 165, respectively). Note: the DREADD hM3Dq exhibits M3 biological activity, but is insensitive to the endogenous ligand acetylcholine (ACh).

化合物21是有效的设计药物,对人hM3Dq具有完全的激动剂活性(通过基于细胞的Ca2 +动员测定,EC50 = 1.7 nM),基于人M3毒蕈碱受体(M3R)的Gq(M3Dq)DREADD(由设计者独家激活的设计受体) 药物),对毒蕈碱型乙酰胆碱受体M3几乎没有活性(在10μM时有30%的M3活化),并且对H1、5HT2A,5HT2C,α1A受体的亲和力降低(选择性分别为3.5、40、100、165)。 注意:DREADD hM3Dq具有M3生物学活性,但对内源性配体乙酰胆碱(ACh)不敏感。

性质

assay  ≥98% (HPLC)
form  powder
storage condition  desiccated
color  yellow to brown
solubility  H2O: 2 mg/mL, clear
storage temp.  −20°C
SMILES string  C1(C=CC=C2)=C2C(N3CCNCC3)=NC(C=CC=C4)=C4N1


安全信息

符号 
GHS07  GHS07
信号词 Warning
危害声明 H302
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16