apratastat manufacturers
- Apratastat
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- $213.00
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2026-05-11
- CAS:287405-51-0
- Purity:
- Supply Ability: 10g
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| | apratastat Basic information |
| Product Name: | apratastat | | Synonyms: | 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) | | CAS: | 287405-51-0 | | MF: | C17H22N2O6S2 | | MW: | 414.5 | | EINECS: | | | Product Categories: | | | Mol File: | 287405-51-0.mol |  |
| | apratastat Chemical Properties |
| 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 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral |
| | apratastat Usage And Synthesis |
| 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 |
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