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CAS: 73573-88-3
分子式: C23H34O5
分子量: 390.51
熔点: 151-153℃
英文名称: 
mevastatin
butanoic acid, 2-methyl-, 1,2,3,7,8,8a-hexahydro-7-methyl-8-(2-(tetrahydro-4-hy
droxy-6-oxo-2h-pyran- 2-yl)ethyl)-1-naphthalenyl ester, (1S-(1-alpha(r*),7-beta
,8-beta(2S*,4S*),8a-beta))-
(+)-compactin
antibiotic ml 236b
compactin
compactin (penicillium)
cs 500
ml 236b lactone
ml-236b
展开更多英文名
推荐供应商
货号品牌产品名称规格包装、参考价格
M795132MACKLIN美伐他汀10mM in DMSO648元/1ml;   咨询
储存:-20°C
M813346MACKLIN美伐他汀≥96%(HPLC)42元/250mg;   60元/1g;   80元/5g;   254元/25g;   900元/100g;   3321元/500g;   咨询
储存:2~8°C
状态:白色到浅黄色粉末
M2275TCIMevastatin>98.0%(HPLC)320元/100MG;   980元/1G;   3290元/5G;   咨询

基本信息

纯度/分析方法>98.0%(HPLC)
分子式/分子量C23H34O5 = 390.52
外观与形状(20℃)固体
储存温度0-10℃
应避免的情况加热
Reaxys-RN3630717
PubChem物质ID135727287
Merck Index (14)6164
MDL编号MFCD05662341

技术规格

AppearanceWhite to Yellow to Orange powder to crystal
Purity(HPLC)min. 98.0 area%
Melting point151.0 to 155.0 ℃
Specific rotation [a]20/D+280 to +295 deg(C=0.4, Acetone)

物性(参考值)

熔点153 ℃
比旋光度 [α]D281° (C=0.4,Acetone)
最大吸收波长246(MeOH) nm

相关法规

RTECS#EK7907100
476082J&KMevastatin98%, 一种竞争性HMG辅酶A(HMG-COA)还原酶抑制剂846元/1G;   咨询

基本信息

分子式C23H34O5
分子量390.51
熔点151.0-155.0
比旋光度([α]20D)+280 to +295
MDL编码MFCD05662341
Beilstein3630717
Merck14,6164
存储条件Freezer -20℃

产品描述

Mevastatin 是竞争性HMG辅酶A(HMG-COA)还原酶抑制剂,比HMG-CoA底物本身结合亲合力高10,000倍。

靶点(IC50 & Targe)

CES1

HMG-CoA reductase

体外研究

Mevastatin是从Penicillium citinium分离出的一种降胆固醇剂。在0.01 pg/mL (26 nM)浓度下,与对照组相比,它能够降低50%的胆固醇合成。[1]它在结构上类似于HMG,一个HMG-CoA还原酶的内源性底物的取代基。Mevastatin是一个前体药物,在体内通过内酯环的水解而活化。水解的内酯环模拟还原酶产生的四面体中间物,使试剂以比天然基底产物高出10,000的亲和力进行结合。mevastatin的二环部分与辅酶A的活性位点结合。Mevastatin增加eNOS mRNA 和蛋白质水平,减少梗死面积,并且剂量时间依赖性提高神经功能缺陷。[2]

体内研究

在5毫克/千克和20毫克/千克剂量下,mevastatin口服给药3小时后会降低血清胆固醇水平。在20毫克/千克的剂量下,它能够降低大约30%的血清胆固醇水平。[1] Mevastatin通过竞争性抑制HMG-CoA还原酶,能够降低肝产生的胆固醇。仅在28天治疗之后,胆固醇水平降低,并且与梗塞减少无关。在14天高剂量治疗后,基线绝对脑血流量高出30%。 [2]

动物实验

Animal Models: Wistar-Imamichi雄性大鼠

Formulation: 生理盐水

Dosages: 5毫克/千克

Administration: 口服

(Only for Reference)

参考文献

[1] Endo A, et al. J Antibiot (Tokyo), 1976, 29(12), 1346-1348.

[2] Amin-Hanjani S, et al. Stroke, 2001, 32(4), 980-986.

安全信息

WGK3
RTECSEK7907100
977126J&KMevastatin96%, 一种竞争性HMG辅酶A(HMG-COA)还原酶抑制剂245元/250MG;   731元/1G;   咨询

基本信息

分子式C23H34O5
分子量390.51
熔点151.0-155.0
比旋光度([α]20D)+280 to +295
MDL编码MFCD05662341
Beilstein3630717
Merck14,6164
存储条件Freezer -20℃

安全信息

WGK3
RTECSEK7907100
R12085Alfa AesarMevastatin,1000ppm1320元/1ml;   咨询

安全信息

危险等级
3

R11048Alfa AesarMevastatin Standard solution100ppm629元/1ml;   咨询

安全信息

危险等级
3

474700Sigma-AldrichMevastatin-CAS 73573-88-3-CalbiochemAn antibiotic that acts as a potent inhibitor of HMG-CoA reductase, thus suppressing Ras farnesylation.1954.93元/50 MG;   咨询

产品说明

一般描述

An antibiotic that acts as a potent inhibitor of HMG-CoA reductase, thus suppressing Ras farnesylation. Inhibitor of myoblast fusion. Also may induce bone morphogenic protein-2 (BMP-2). Causes cell cycle arrest in late G1 phase.
This is an inactive form which may require activation for use with isolated cells depending upon the application. To activate, treat with NaOH in ethanol and then neutralize to pH 7.2.
An antibiotic that acts as a potent inhibitor of HMG-CoA reductase, thus suppresses Ras farnesylation. Inhibitor of myoblast fusion. Causes cell cycle arrest in late G1 phase. May induce bone morphogenic protein-2 (BMP-2). This product requires activation for use in cell culture and cell-free assay systems. To activate, treat with ethanol solution with 1 N NaOH and then neutralize with 1 N HCl to pH 7.2 (see Keyomarsi, K . et al. 1991).

包装

50 mg in Plastic ampoule

生化/生理作用

Primary Target
HMG-CoA reductase
Product does not compete with ATP.
Reversible: no
Cell permeable: no

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

其他说明

Sugiyama, M., et al. 2000. Biochem. Biophys. Res. Commun.271, 688.
Hug, T., et al. 1995. Pflugers Archiv. Eur. J. Physiol.429, 682.
Belo, R.S., et al. 1993. Mol.Cell. Biochem.126, 159.
McLeish, K.R., et al. 1993. Biochem. Biophys. Res. Commun.197, 763.
Keyomarsi, K., et al. 1991. Cancer Res. 51, 3602.
Jackson, J.H., et al. 1990. Proc. Natl. Acad. Sci. USA 87, 3042.
Kita, T., et al. 1980. J. Clin. Invest. 66, 1094.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C23H34O5
分子量390.51
MDL编号MFCD05662341

产品性质

质量水平100
测定≥95% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
颜色 white
溶解性ethanol: soluble
运输ambient
储存温度2-8℃
InChI1S/C23H34O5/c1-4-14(2)23(26)28-20-7-5-6-16-9-8-15(3)19(22(16)20)11-10-18-12-17(24)13-21(25)27-18/h6,8-9,14-15,17-20,22,24H,4-5,7,10-13H2,1-3H3/t14-,15-,17+,18+,19-,20-,22-/m0/s1
InChI keyAJLFOPYRIVGYMJ-INTXDZFKSA-N

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
M2537Sigma-AldrichMevastatin≥98% (HPLC), powder or crystals1779.35元/5 MG;   咨询

产品说明

一般描述

美伐他汀(Mevastatin)是一种聚酮,属于他汀类化合物。结构中含有一个羟基-六氢萘环。
化学结构:他汀

应用

美伐他汀已用于:

  • 通过细胞毒性检测分析其对慢性淋巴细胞白血病(CLL)细胞的影响
  • 分析其作为异戊二烯化抑制剂,对K-Ras转染人胚胎肾细胞(HEK)的影响
  • 研究其作为他汀类药物,对人乳腺癌细胞和胶质母细胞瘤的体外抗癌作用

生化/生理作用

美伐他汀是一种参与胆固醇合成的主要酶——3-羟基3-甲戊二酰辅酶A还原酶(HMG-CoA还原酶)的选择性抑制剂,可用作降胆固醇药。美伐他汀来源于各种真菌。美伐他汀可作为抗骨吸收剂,对骨质疏松症有治疗作用。可通过诱发破骨细胞凋亡抑制骨吸收。美伐他汀也参与蛋白质(如Ras)异戊二烯化的抑制。可通过抑制转录因子Rho的四异戊二烯化,提高内皮一氧化氮合酶(eNOS)mRNA和蛋白质水平。

特点和优势

该化合物由 第一三共制药开发。要浏览其他制药公司开发的化合物列表批准的药物/候选药物的列表, 点击这里 。

包装

无底玻璃瓶。内含物装在插入的融合锥内。

基本信息

经验(实验)分子式C23H34O5
分子量390.51
Beilstein1269441
MDL编号MFCD05662341
PubChem化学物质编号24278540
NACRESNA.77

产品性质

质量水平200
测定≥98% (HPLC)
形式powder or crystals
颜色 white to light yellow
mp151  ℃
溶解性ethanol: 25-26 mg/mL, clear, colorless
作用机制enzyme | inhibits
抗生素抗菌谱neoplastics
创始人Daiichi-Sankyo
储存温度2-8℃
SMILES string[H][C@]12[C@H](CCC=C1C=C[C@H](C)[C@@H]2CC[C@@H]3C[C@@H](O)CC(=O)O3)OC(=O)[C@@H](C)CC
InChI1S/C23H34O5/c1-4-14(2)23(26)28-20-7-5-6-16-9-8-15(3)19(22(16)20)11-10-18-12-17(24)13-21(25)27-18/h6,8-9,14-15,17-20,22,24H,4-5,7,10-13H2,1-3H3/t14-,15-,17+,18+,19-,20-,22-/m0/s1
InChI keyAJLFOPYRIVGYMJ-INTXDZFKSA-N
Gene Informationhuman ... HMGCL(3155), HMGCR(3156)
rat ... Hmgcr(25675)

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
个人防护装备Eyeshields, Gloves, type N95 (US)
PHR2240SupelcoMevastatin/Lovastatin Impurity APharmaceutical Secondary Standard; Certified Reference Material2222.07元/50 MG;   咨询

产品说明

一般描述

Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

分析说明

These secondary standards offer multi-traceability to the USP, EP and BP primary standards, where they are available.

其他说明

This Certified Reference Material (CRM) is produced and certified in accordance with ISO 17034 and ISO/IEC 17025. All information regarding the use of this CRM can be found on the certificate of analysis.

附注

To see an example of a Certificate of Analysis for this material enter LRAC3412 in the Documents slot below. This is an example certificate only and may not be the lot that you receive.

基本信息

经验(实验)分子式C23H34O5
分子量390.51
Beilstein1269441
MDL编号MFCD05662341

产品性质

等级certified reference material
pharmaceutical secondary standard
形式solid
包装pkg of 50 mg
储存温度-10 to -25℃
SMILES string[H][C@]12[C@H](CCC=C1C=C[C@H](C)[C@@H]2CC[C@@H]3C[C@@H](O)CC(=O)O3)OC(=O)[C@@H](C)CC
InChI1S/C23H34O5/c1-4-14(2)23(26)28-20-7-5-6-16-9-8-15(3)19(22(16)20)11-10-18-12-17(24)13-21(25)27-18/h6,8-9,14-15,17-20,22,24H,4-5,7,10-13H2,1-3H3/t14-,15-,17+,18+,19-,20-,22-/m0/s1
InChI keyAJLFOPYRIVGYMJ-INTXDZFKSA-N

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
M02108FluorochemMevastatin>95%1650元/1g;   5588元/5g;   咨询

基本信息

CAS Number73573-88-3
MDL NumberMFCD05662341

安全信息

图形或危害标志
危险性说明 H315: Causes skin irritation.
H319: Causes serious eye irritation.
H335: May cause respiratory irritation.
防范说明 P233: Keep container tightly closed.
P260: Do not breathe .
P261: Avoid breathing .
P264: Wash hands thoroughly after handling.
P271: Use only outdoors or in a well-ventilated area.
P280: Wear .
P302 + P352: IF ON SKIN: Wash with plenty of soap and water.
P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing..
P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P312: Call a POISON CENTER or doctor/physician if you feel unwell.
P321: Specific treatment (see relevant procedures. on this label).
P332 + P313: If skin irritation occurs: Get medical advice/ attention.
P337 + P313: If eye irritation persists: Get medical advice/attention.
P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P362: Take off contaminated clothing and wash before reuse.
P403: Store in a well-ventilated place.
P403 + P233: Store in a well-ventilated place. Keep container tightly closed.
P405: Store locked up.
P501: Dispose of contents/container to in accordance with local regulation .
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