apratastat

Product Name: apratastat
CAS No.: 287405-51-0
Chemical Name: apratastat
Synonyms: TMI 005;apratastat;TMI 005 - Apratastat;Apratastat >=98% (HPLC);N-hydroxy-4-[[4-[(4-hydroxy-2-butynyl)oxy]phenyl]sulfonyl]-2,2-dimethyl-3-thiomorpholinecarboxamide;3-Thiomorpholinecarboxamide, N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-, (3S)-
CBNumber: CB81508587
Molecular Formula: C17H22N2O6S2
Formula Weight: 414.5
MOL File: 287405-51-0.mol

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apratastat Property

Density: 1.390
storage temp.: Store at -20°C
solubility: DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS (pH 7.2) (1:40): 0.02 mg/ml; Ethanol: 10 mg/ml
form: A crystalline solid
pka: 9.25±0.23(Predicted)
color: White to off-white
InChI: 1S/C17H22N2O6S2/c1-17(2)15(16(21)18-22)19(9-12-26-17)27(23,24)14-7-5-13(6-8-14)25-11-4-3-10-20/h5-8,15,20,22H,9-12H2,1-2H3,(H,18,21)/t15-/m0/s1
InChIKey: MAVDNGWEBZTACC-HNNXBMFYSA-N
SMILES: O=S(N1CCSC(C)(C)[C@@H]1C(NO)=O)(C2=CC=C(OCC#CCO)C=C2)=O

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Safety

WGK Germany: WGK 3
Storage Class: 11 - Combustible Solids
Hazard Classifications: Acute Tox. 4 Oral

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning
Hazard statements: H302Harmful if swallowed

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1543
Product name: Apratastat
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $227
Updated: 2026/03/19

Sigma-Aldrich

Product number: SML1543
Product name: Apratastat
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $718
Updated: 2026/03/19

Cayman Chemical

Product number: 29016
Product name: TMI-005
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 29016
Product name: TMI-005
Packaging: 10mg
Price: $341
Updated: 2024/03/01

Cayman Chemical

Product number: 29016
Product name: TMI-005
Packaging: 5mg
Price: $183
Updated: 2024/03/01

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apratastat Chemical Properties,Usage,Production

Uses

Treatment of rheumatoid arthritis.

Definition

ChEBI: Apratastat is a sulfonamide.

brand name

(Wyeth).

Biological Activity

Apratast at (TMI-005) is an orally active, potent and selective dual inhibitor of disintegrin metalloenzyme 17 (ADAM17/ TACE) and matrix metalloprotease (MMP).

in vivo

Apratastat (10 mg/kg, i.p., administered twice at 4 and 16 hours post-induction) alleviats lung inflammation induced by Poly(I ) (HY-119307) and SARS-CoV-2 RBD-S protein in C57BL/6 mice^[3]. Apratastat (10 mg/kg, p.o., once daily for 14 days) exhibits anti-tumor and anti-angiogenic activity in the MC38 xenograft C57BL/6 mouse model^[4].

Animal Model:	Poly(I ) (HY-107202) and SARS-CoV-2 RBD-S protein-induced lung inflammation model in C57BL/6 mice^[3]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (i.p.), administered twice at 4 and 16 hours post-surgery
Result:	Significantly reduced neutrophil and macrophage numbers in lung tissue, improved lung tissue morphology.

Animal Model:	MC38 colorectal cancer cell xenograft model in C57BL/6 mice^[4]
Dosage:	10 mg/kg
Administration:	Oral gavage (p.o.), once daily for 14 days
Result:	Significantly inhibited tumor growth, reduced tumor angiogenesis and lymphangiogenesis.

IC 50

MMP

apratastat Preparation Products And Raw materials

Raw materials

Preparation Products

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apratastat Suppliers

China 25 The Netherlands 1 United States 7 Global 33

Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
ProdList: 9803
Advantage: 58

Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840 18892239720
Fax: 010-60605840
Email: psaitong@jm-bio.com
Country: China
ProdList: 12306
Advantage: 58

Amatek Scientific Co. Ltd.

Tel: 0512-56316828
Fax: 0512-56316826
Email: info@amateksci.com
Country: China
ProdList: 28774
Advantage: 58

Fan De(Beijing) Biotechnology Co., Ltd.

Tel: 15911056312
Email: liming@bio-fount.com
Country: China
ProdList: 9729
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354; +17819995354
Email: marketing@targetmol.com
Country: United States
ProdList: 32469
Advantage: 58

Energy Chemical

Tel: 021-58432009 400-005-6266
Fax: 021-58436166
Email: marketing@energy-chemical.com
Country: China
ProdList: 44918
Advantage: 58

cjbscvictory

Tel: 13348960310 13348960310;
Email: 3003867561@qq.com
Country: China
ProdList: 10503
Advantage: 58

Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840 15801484223;
Email: psaitong@jm-bio.com
Country: China
ProdList: 29757
Advantage: 58

TargetMol Chemicals Inc.

Tel: 4008200310
Email: marketing@tsbiochem.com
Country: China
ProdList: 24962
Advantage: 58

Suzhou Meishi Biotechnology Co., Ltd.

Tel: 1173954148q
Email: meishipharma@126.com
Country: China
ProdList: 20033
Advantage: 58

287405-51-0, apratastatRelated Search:

apratastat

TMI 005 - Apratastat

N-hydroxy-4-[[4-[(4-hydroxy-2-butynyl)oxy]phenyl]sulfonyl]-2,2-dimethyl-3-thiomorpholinecarboxamide

TMI 005

3-Thiomorpholinecarboxamide, N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-, (3S)-

Apratastat >=98% (HPLC)

287405-51-0