Cas(50-35-1), Thalidomide-阿拉丁试剂, 沙利度胺,Thalidomide,

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货号 (SKU)	包装规格	是否现货
T126856-250mg	250mg	现货
T126856-1g	1g	现货
T126856-5g	5g	现货
T126856-25g	25g	现货
T126856-100g	100g	现货

货号 (SKU)

包装规格

是否现货

价格

数量

T126856-250mg

250mg

现货

T126856-1g

现货

T126856-5g

现货

T126856-25g

25g

现货

T126856-100g

100g

现货

基本描述

规格或纯度	≥98%
英文名称	Thalidomide
别名	沙利度胺；(±)-2-（2,6-二氧代-3-哌啶基）-1H-异吲哚-1,3 (2H)-二酮；(±)-Thalidomide; N-(2,6-二氧-3-哌啶基)邻苯二甲酰亚胺
英文别名	(±)-2-(2,6-Dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione;N-(2,6-Dioxo-3-piperidinyl)phthalimide;(±)-Thalidomide；N-(2,6-Dioxo-3-piperidinyl)phthalimide
生化机理	Thalidomide was commonly used therapeutically in the late 1950’s, however, it was withdrawn from the market when it was discovered to cause birth defects. More recent research has found Thalidomide to affect key biochemical pathways yielding antiangiogenic and immunomodulatory activities. This compound has been shown to: selectively inhibit TNF α (tumor necrosis factor-α) biosynthesis and basic fibroblast growth factor (bFGF)-induced angiogenesis, induce apoptosis in human monocytes via a cytochrome c-dependent pathway, and to inhibit HIV-1 replication in a monocytoid (U1) line. These new found uses make Thalidomide an extremely valuable research tool.Immunomodulator. Antiproliferative, antiangiogenic and pro-apoptotic.
运输条件	常规运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	应用：沙利度胺已被用于阿尔茨海默病 (AD) 小鼠模型的神经病理学研究。该研究报道，长期服用沙利度胺可引起 β-分泌酶抑制，继而减轻类淀粉样病理。此外，沙利度胺也被用于评价其致畸功能。沙利度胺可影响人胚胎干细胞和诱导多能干细胞分化过程中的内胚层分化和神经发育。 A selective inhibitor of TNF alpha biosynthesis shown to have immunomodulatory and antiangeogenic activity.

名称和标识符

EC号	200-031-1
IUPAC Name	2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
INCHI	InChI=1S/C13H10N2O4/c16-10-6-5-9(11(17)14-10)15-12(18)7-3-1-2-4-8(7)13(15)19/h1-4,9H,5-6H2,(H,14,16,17)
InChi Key	UEJJHQNACJXSKW-UHFFFAOYSA-N
Canonical SMILES	C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
分子式	C₁₃H₁₀N₂O₄
UN Number	2811
PubChem CID	5426
分子量	258.23

数据库链接

DrugBank Ligand	DB01041
PubChem CID	5426
CAS Registry No.	50-35-1
ChEMBL Ligand	CHEMBL468
Wikipedia	Thalidomide
Immunopaedia Search	thalidomide
Reactome Reaction	R-HSA-9681169
Reactome Drug	R-ALL-9681254
DrugCentral Ligand	2616

化学和物理性质

溶解性	Soluble in DMSO (>25 mg/ml), cold pyridine, dimethylformamide, dioxane, Acetone, Butyl Acetate, Ethanol (≥2 mg/ml), Ethyl Acetate, Methanol, water (<1 mg/mL ), and 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (0.6 mg/mL).
熔点	276 °C

安全信息

象形图	Health Hazard Harmful
信号词	Danger
危险声明	H302: Harmful if swallowed H360: May damage fertility or the unborn child
预防措施声明	P280,P405,P501,P264,P270,P330,P203,P301+P317,P318
WGK Germany	3
RTECS	TI4375000
Merck Index	9255
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

靶标

Target ID

3086

名称

cereblon

缩写名

SHP2

家族

E3 ubiquitin ligase components

别名

IRK2

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	442	3p26.2	CRBN	cereblon
Mouse	2	445	6 E1	Crbn	cereblon
Rat	2	445	4q41	Crbn	cereblon

Ensembl Gene

ENSG00000113851 (Hs) , ENSMUSG00000005362 (Mm) , ENSRNOG00000006534 (Rn)

UniProtKB

Q96SW2 (Hs) , Q8C7D2 (Mm) , Q56AP7 (Rn)

RefSeq Protein

NP_057386 (Hs) , NP_780566 (Mm) , NP_001015003 (Rn)

Protein GI

39545580 (Hs) , 28202023 (Mm) , 62543497 (Rn)

RefSeq Nucleotide

NM_016302 (Hs) , NM_175357 (Mm) , NM_001015003 (Rn)

OMIM

609262 (Hs)

Entrez Gene

51185 (Hs) , 58799 (Mm) , 297498 (Rn)

ChEMBL Target

CHEMBL3763008 (Hs)

关联配体

Ligand ID	7327
名称	thalidomide
别名	K-17
类别	Synthetic organic
学名	2-(6-hydroxy-2-oxo-2,3,4,5-tetrahydropyridin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	Thalidomide is principally an immunomodulatory drug. It inhibits synthesis of TNFα. Mechanistically, thalidomide binds to cereblon, and this complex recruits substrate proteins for degradation by the ubiquitin system. The lymphoid transcription factors Ikaros (IKZF1) and Aiolos (IKZF3) have been identified as substrates for thalidomide-bound cereblon. More recently another transcription factor, PLZF (ZBTB16), has been reported as a potential thalidomide/cereblon substrate . Knockdown of Plfz induces skeletal abnormalities in chicken limbs, so thalidomide-targeted degradation of PLZF would be predicted to exhibit similar teratogenic effects. SARS-CoV-2 and COVID-19: Thalidomide + low-dose glucocorticoid is being evaluated for efficacy in severe COVID-19 pneumonia (preprint available here https://www.preprints.org/manuscript/202002.0395/v1). An alternative approach is examining the combination of thalidomide + celecoxib (which targets NF-κB to suppress production of inflammatory cytokines; see preprint DOI: 10.13140/RG.2.2.26979.91689).
配体家族	PROTACs, molecular glues and other degraders

参考文献

1. Xin W, Xiaohua N, Peilin C, Xin C, Yaqiong S, Qihan W. (2008) Primary function analysis of human mental retardation related gene CRBN.. Mol Biol Rep, 35 (2): (251-6). [PMID:17380424]
2. Jo S, Lee KH, Song S, Jung YK, Park CS. (2005) Identification and functional characterization of cereblon as a binding protein for large-conductance calcium-activated potassium channel in rat brain.. J Neurochem, 94 (5): (1212-24). [PMID:16045448]
3. Ito T, Ando H, Suzuki T, Ogura T, Hotta K, Imamura Y, Yamaguchi Y, Handa H. (2010) Identification of a primary target of thalidomide teratogenicity.. Science, 327 (5971): (1345-50). [PMID:20223979]
4. Lopez-Girona A, Mendy D, Ito T, Miller K, Gandhi AK, Kang J, Karasawa S, Carmel G, Jackson P, Abbasian M et al.. (2012) Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.. Leukemia, 26 (11): (2326-35). [PMID:22552008]
5. Mazzoccoli L, Cadoso SH, Amarante GW, de Souza MV, Domingues R, Machado MA, de Almeida MV, Teixeira HC. (2012) Novel thalidomide analogues from diamines inhibit pro-inflammatory cytokine production and CD80 expression while enhancing IL-10.. Biomed Pharmacother, 66 (5): (323-9). [PMID:22770990]
6. Eichner R, Heider M, Fernández-Sáiz V, van Bebber F, Garz AK, Lemeer S, Rudelius M, Targosz BS, Jacobs L, Knorn AM et al.. (2016) Immunomodulatory drugs disrupt the cereblon-CD147-MCT1 axis to exert antitumor activity and teratogenicity.. Nat Med, 22 (7): (735-43). [PMID:27294876]
7. Quayle LA et al.. (2017) Anti-angiogenic drugs: direct anti-cancer agents with mitochondrial mechanisms of action.. Oncotarget, 8 (51): (88670-88688). [PMID:29179466]
8. Rosa TLSA et al.. (2022) The Type I Interferon Pathway Is Upregulated in the Cutaneous Lesions and Blood of Multibacillary Leprosy Patients With Erythema Nodosum Leprosum.. Front Med (Lausanne), 9 (): (899998). [PMID:35733868]

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(±)-沙利度胺

库存信息

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

安全信息

靶标

关联配体

参考文献

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(±)-沙利度胺

库存信息

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

安全信息

靶标

关联配体

参考文献

相关文档

质检报告COA

产品问答

产品问答

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