< 生产厂家价格 >

(R)-(+)-沙利度胺

(R)-(+)-沙利度胺用途

(R)-Thalidomide ((R)-(+)-Thalidomide) 是 Thalidomide 的 R-对映异构体。(R)-Thalidomide 具有镇静作用。

点击显示

(R)-(+)-沙利度胺名称

[ CAS 号 ]:
2614-06-4

[ 中文名 ]:
(+)-沙利度胺

[ 英文名 ]:
(R)-(+)-Thalidomide

[中文别名 ]:

[英文别名 ]:

(+)-Thalidomide
MFCD00210220
(R)-(+)-Thalidomide

(R)-(+)-沙利度胺生物活性

[ 描述 ]:

(R)-Thalidomide ((R)-(+)-Thalidomide) 是 Thalidomide 的 R-对映异构体。(R)-Thalidomide 具有镇静作用。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 代谢疾病

[体外研究]

由于沙利度胺在有机相中的较强保留作用,沙利度胺从R-印迹MIP-1经供体相到受体相的转运要少得多。与(R)-沙利度胺的亲和力相比,MIP具有更强的表面捕获能力。在(R)-沙利度胺的情况下,发现它与MIP的选择位点结合的强度比反映其不同生物实体的另一个更强[1]。(S)-沙利度胺印迹MIP纳米粒子对Caco-2细胞产生的细胞毒性作用大于(R)-沙利度胺印迹MIPS〔1〕。

[体内研究]

成年雌性F344大鼠在颅内、皮下(侧面)或两者同时植入9L胶质肉瘤肿瘤。治疗数周后,评估口服沙利度胺和腹腔BCNU或顺铂联合化疗的疗效。(R)-沙利度胺的血清和组织浓度均比(S)-沙利度胺高40-50%。BCNU或顺铂与沙利度胺的联合给药不会改变浓度对映选择性[1]。

[参考文献]

[1]. Murphy S, et al. Enantioselectivity of thalidomide serum and tissue concentrations in a rat glioma model and effects of combination treatment with cisplatin and BCNU. J Pharm Pharmacol. 2007 Jan;59(1):105-14.

[2]. Eriksson T, et al. Intravenous formulations of the enantiomers of thalidomide: pharmacokinetic and initial pharmacodynamic characterization in man. J Pharm Pharmacol. 2000 Jul;52(7):807-17.

(R)-(+)-沙利度胺物理化学性质

[ 密度 ]:
1.503g/cm3

[ 沸点 ]:
509.7ºC at 760 mmHg

[ 熔点 ]:
269-271ºC

[ 分子式 ]:
C₁₃H₁₀N₂O₄

[ 分子量 ]:
258.22900

[ 闪点 ]:
262.1ºC

[ 精确质量 ]:
258.06400

[ PSA ]:
83.55000

[ LogP ]:
0.35450

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
1.65E-10mmHg at 25°C

[ 折射率 ]:
1.646

[ 储存条件 ]:
-20°C

(R)-(+)-沙利度胺MSDS

(R)-(+)-沙利度胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TI4925000

CHEMICAL NAME :: Phthalimide, N-(2,6-dioxo-3-piperidyl)-, D-(+)-

CAS REGISTRY NUMBER :: 2614-06-4

LAST UPDATED :: 199012

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C13-H10-N2-O4

MOLECULAR WEIGHT :: 258.25

WISWESSER LINE NOTATION :: T56 BVNVJ C- DT6VMVTJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 215,296,1967 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 50 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 29,1640,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 900 mg/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

REFERENCE :: NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 215,296,1967 *** REVIEWS *** TOXICOLOGY REVIEW BCSTB5 Biochemical Society Transactions. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1973- Volume(issue)/page/year: 2,695,1974

点击显示

(R)-(+)-沙利度胺安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H360

[ 警示性声明 ]:
P201-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R61

[ 安全声明 (欧洲) ]:
S45;S53;S36/S37/S39

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
TI4925000

[ 海关编码 ]:
2925190090

(R)-(+)-沙利度胺合成路线

(R)-(+)-沙利度胺上下游产品

(R)-(+)-沙利度胺上游产品

(R)-(+)-沙利度胺下游产品

(R)-(+)-沙利度胺海关

[ 海关编码 ]: 2925190090

[ 中文概述 ]:
2925190090 其他酰亚胺及其衍生物盐. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2925190090 other imides and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

(R)-(+)-沙利度胺文献

Thalidomide is an inhibitor of angiogenesis.

Proc. Natl. Acad. Sci. U. S. A. 91 , 4082, (1994)

Thalidomide is a potent teratogen causing dysmelia (stunted limb growth) in humans. We have demonstrated that orally administered thalidomide is an inhibitor of angiogenesis induced by basic fibroblas...

Thalidomide inhibits the replication of human immunodeficiency virus type 1.

Proc. Natl. Acad. Sci. U. S. A. 90 , 5974-5878, (1993)

Thalidomide, a selective inhibitor of tumor necrosis factor alpha (TNF-alpha) synthesis, suppresses the activation of latent human immunodeficiency virus type 1 (HIV-1) in a monocytoid (U1) line. The ...

Thalidomide induces limb anomalies by PTEN stabilization, Akt suppression, and stimulation of caspase-dependent cell death.

Mol. Cell. Biol. 28(2) , 529-538, (2008)

Thalidomide, a drug used for the treatment of multiple myeloma and inflammatory diseases, is also a teratogen that causes birth defects, such as limb truncations and microphthalmia, in humans. Thalido...

更多文献