|(2'R,3S,3'R,3a'S,6aS,6bS,6'S,7a'R,11aS,11bR)-3-羟基-3',6',10,11b-四甲基-1,3,3a' ,4,4',5',6,6a,6b,6',7,7',7a',8,11a,11b-十六氢-3'H-螺[苯并[a]芴-9,2' -呋喃并[3,2-b]吡啶] -11(2H)-酮|CsnPharm

CAS No.: 469-59-0

蒜黎芦碱 Catalog No. CSN15980

Synonyms: 11-Ketocyclopamine;NSC 7520;NSC 23898

Jervine is hedgehog signaling inhibitor with IC50 of 500 nM-700 nM that disrupts the interaction with smoothened.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Hedgehog

IC50:500-700nM
描述Hedgehog (Hh) is one of few of signaling pathways that is frequently used during development for intercellular communication. Hh is important for the organ oogenesis of almost all organs in mammals, as well as in regeneration and homeostasis. Further, Hh signaling is disrupted in diverse types of cancer. Jervine, also called 11-Ketocyclopamine, is hedgehog signaling inhibitor with IC₅₀ of 500 - 700 nM. Tongues cultured with 5 μM cyclopamine or jervine had an increased density of fungiform papillae on the anterior tongue, and numerous fungiform papillae on the posterior tongue near the circumvallate papilla, compared with 5 μM solanidine-treated group^[5]. Oral administration of jervine (50-400 mg/kg) exerted 50.4-73.5% anti-inflammatory effects in carrageenan induced paw edema and inflammation biomarkers such as TNF-α, IL-1β and MPO that increased by carrageenan injection were suppressed by the administrations of all doses of jervine^[6]. It was found that jervine significantly increased external granule layer (proliferative layer producing over 90% of cerebellar neurons) apoptosis at 50 mg/kg and above in a dose dependent manner^[7].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
s12 cells	-	Function assay	-	Inhibition of lipid-modified (octylated) form of SHH expressed in mouse s12 cells by luciferase reporter gene assay, IC50=0.5 μM	19309080

动物研究

剂量

Rat: 5 mg/kg^[2] (p.o.), 50 mg/kg - 400 mg/kg^[3] (p.o.); 1.5 mg/kg^[4] (i.v.)

给药途径

p.o., i.v.

动物药代数据

Animal	Rats^[4]
Dose	1.5 mg/kg
Administration	i.v.
MRT_0→t	3.2 ± 0.6 h
T_1/2z	3.4 ± 1.2 h
V_z/F	8.1 ± 4.0 L/kg
CL_z/F	1.7 ± 0.5 L/h/kg
C_max	506.6 ± 192.8 ng/ml
AUC_0→∞	969.3 ± 277.7 ng/ml·h
MRT_0→∞	4.4 ± 1.5 h
AUC_0→t	892.6 ± 285.0 ng/ml·h

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3496 mL
- 11.7480 mL
- 23.4960 mL
- 5 mM
- 0.4699 mL
- 2.3496 mL
- 4.6992 mL
- 10 mM
- 0.2350 mL
- 1.1748 mL
- 2.3496 mL

技术信息

CAS号

469-59-0

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H39NO3

运输

蓝冰

分子量

425.60

别名

11-Ketocyclopamine;NSC 7520;NSC 23898;蒜黎芦碱;蒜藜芦碱

溶解度

DMSO	5.0 mg/mL (11.7 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (4.7 mM)

动物实验配方

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靶点选择性

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