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蒜黎芦碱 /Jervine {[allProObj[0].p_purity_real_show]}

货号:A160362 同义名: 蒜藜芦碱 / 11-Ketocyclopamine;NSC 7520

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

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Jervine 化学结构 CAS号:469-59-0
Jervine 化学结构
CAS号:469-59-0
Jervine 3D分子结构
CAS号:469-59-0
Jervine 化学结构 CAS号:469-59-0
Jervine 3D分子结构 CAS号:469-59-0
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Jervine 纯度/质量文件 产品仅供科研

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Jervine 生物活性

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].

Jervine 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
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

Jervine 动物研究

Dose Rat: 5 mg/kg[2] (p.o.), 50 mg/kg - 400 mg/kg[3] (p.o.); 1.5 mg/kg[4] (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Rats[4]
Dose 1.5 mg/kg
Administration i.v.
MRT0→t 3.2 ± 0.6 h
T1/2z 3.4 ± 1.2 h
Vz/F 8.1 ± 4.0 L/kg
CLz/F 1.7 ± 0.5 L/h/kg
Cmax 506.6 ± 192.8 ng/ml
AUC0→∞ 969.3 ± 277.7 ng/ml·h
MRT0→∞ 4.4 ± 1.5 h
AUC0→t 892.6 ± 285.0 ng/ml·h

Jervine 参考文献

[1]Campbell M, Horton W, Keeler R. Comparative effects of retinoic acid and jervine on chondrocyte differentiation. Teratology. 1987 Oct;36(2):235-43.

[2]Yakan S, Aydin T, et al. The protective role of jervine against radiation-induced gastrointestinal toxicity. J Enzyme Inhib Med Chem. 2019 Dec;34(1):789-798.

[3]Dumlu FA, Aydin T, et al. Anti-inflammatory and antioxidant properties of jervine, a sterodial alkaloid from rhizomes of Veratrum album. Phytomedicine. 2019 Mar 1;55:191-199.

[4]Chen L, Weng Q, et al. A New UPLC-MS/MS Method Validated for Quantification of Jervine in Rat Plasma and the Study of Its Pharmacokinetics in Rats. J Anal Methods Chem. 2019 Mar 7;2019:5163625.

[5]Mistretta CM, Liu HX, Gaffield W, MacCallum DK. Cyclopamine and jervine in embryonic rat tongue cultures demonstrate a role for Shh signaling in taste papilla development and patterning: fungiform papillae double in number and form in novel locations in dorsal lingual epithelium. Dev Biol. 2003 Feb 1;254(1):1-18. doi: 10.1016/s0012-1606(02)00014-3. PMID: 12606278.

[6]Dumlu FA, Aydin T, Odabasoglu F, Berktas OA, Kutlu Z, Erol HS, Halici MB, Cadirci E, Cakir A. Anti-inflammatory and antioxidant properties of jervine, a sterodial alkaloid from rhizomes of Veratrum album. Phytomedicine. 2019 Mar 1;55:191-199. doi: 10.1016/j.phymed.2018.06.035. Epub 2018 Aug 11. PMID: 30668429.

[7]Noguchi KK, Cabrera OH, Swiney BS, Salinas-Contreras P, Smith JK, Farber NB. Hedgehog regulates cerebellar progenitor cell and medulloblastoma apoptosis. Neurobiol Dis. 2015 Nov;83:35-43. doi: 10.1016/j.nbd.2015.08.020. Epub 2015 Aug 28. PMID: 26319366; PMCID: PMC4674325.

Jervine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.75mL

2.35mL

1.17mL

23.50mL

4.70mL

2.35mL

Jervine 技术信息

CAS号469-59-0
分子式C27H39NO3
分子量 425.603
别名 蒜藜芦碱 ;11-Ketocyclopamine;NSC 7520;NSC 23898
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 1 mg/mL(2.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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