Mevastatin (Compactin) CAS: 73573-88-3
MF: C23H34O5
MW: 390.5
An HMGCR (HMG-CoA reductase) inhibitor.

Mevastatin (Compactin) (CAS 73573-88-3)

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Synonym: Compactin
Application An HMGCR (HMG-CoA reductase) inhibitor
CAS 등록번호: 73573-88-3
순도: ≥97%
분자량: 390.5
분자식: C23H34O5
* 참조분석증명서대량의 측정 데이터(함수량포함).
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Mevastatin (Compactin) inhibits HMGCR (HMG-CoA reductase) (Ki for acid form is 1 nM) which in turn inhibits isoprenoid biosynthesis and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans. Mevastatin causes cells to arrest early in the G1 phase. Mevastatin is a close structural analog of lovastatin (sc-200850) and both agents have the same biochemical and pharmacological activities. Mevastatin is inactive in cell-free assays. In cells however, it is hydrolyzed to the active free acid form by intracellular esterases.


References

1. Quesney-Huneeus, V., et al. 1979. Proc. Natl. Acad. Sci. U.S.A. 76: 5056-5060. PMID: 291922
2. Quesney-Huneeus, V., et al. 1983. J. Biol. Chem. 258: 378-385. PMID: 6848509
3. Evangelopoulos, M.E., et al. 2009. J. Neurosci. Res. 87: 2138-2144. PMID: 19224573
4. Sugazaki, M., et al. 2010. Connect. Tissue Res. 51: 105-112. PMID: 20109072

Physical State :
Solid
용해도 :
Soluble in water (Partly miscible), acetone, DMSO (20 mg/ml), 100% ethanol (25 mg/ml), 1:1 ethanol:PBS(pH7.2) (0.5 mg/ml), and DMF (~5 mg/ml).
저장 :
Store at -20° C
녹는점 :
152° C
비등점 :
555.01° C at 760 mmHg (Predicted)
밀도 :
1.13 g/cm3 at 20° C
굴절률 :
n20D 1.54 (Predicted)
Optical Activity :
α22/D +283°, c = 0.48 in acetone
IC50 :
TNF-induced NF-κB activation: IC50 = ~17 µM (human myeloid leukemia cells); HMG-CoA reductase: IC50 = 10 nM (rat); HMG-CoA reductase: IC50 = 23 nM (human)
Ki 데이타 :
HMG-CoA reductase: Ki(for acid form) = 1 nM (human)
pK Values :
pKa: 13.49
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
WGK Germany :
3
RTECS :
EK7907100
PubChem CID :
64715
Merck Index :
14: 6164
MDL Number :
MFCD05662341
Beilstein Registry :
1269441

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분석증명서

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Mevastatin (Compactin)  논문정보

다른 사용자의 Mevastatin (Compactin)사용법보기. 클릭하여 PubMed entry보기 .

Citations 1 to 10 of {3} total

PMID: # 26344763  Gabitova, L. et al. 2015. Cell Rep. 12: 1927-38.

PMID: # 26608317  Cuesta-Geijo, MÁ. et al. 2015. J. Virol. 90: 1534-43.

PMID: # 24954548  Harrison, AT. et al. 2015. Chem Biol Drug Des. 85: 290-5.

PMID: # 25188024  Bozza, WP. et al. 2014. PLoS ONE. 9: e107010.

PMID: # 19903814  Vukelic, S. et al. 2010. J. Biol. Chem. 285: 1980-1988.

PMID: # 17485462  Ko, MH. et al. 2007. J. Biol. Chem. 282: 19742-19752.

PMID: # 16407252  Senga, T. et al. 2006. J. Biol. Chem. 281: 6246-6252.

PMID: # 16428899  Crespo, MJ. et al. 2006. Pharmacology. 76: 141-147.

PMID: # 16043642  Sen-Banerjee, S. et al. 2005. Circulation. 112: 720-726.

PMID: # 12952856  Zager, RA. et al. 2003. Am. J. Physiol. Renal Physiol. 285: F1092-F1099.

Citations 1 to 10 of {3} total
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