Sebetralstat free base
Sebetralstat, also known as KVD-900, is a fast-acting oral PKa inhibitor that rapidly inhibits PKa activity, kallikrein kinin system activation and HK cleavage in plasma. On-demand administration of KVD900 may provide an opportunity to halt the generation of bradykinin and reverse HAE attacks. KVD900 is a selective, competitive and reversible inhibitor of human PKa enzyme with a Ki of 3.02 nM. The association constant (Kon ) of KVD900 for PKa is >10 × 106 M-1 s-1 .
For research use only. We do not sell to patients.
Chemical Information
| Name | Sebetralstat free base |
|---|---|
| Iupac Chemical Name | N-[(3-Fluoro-4-methoxypyridin-2-yl)methyl]-3-methoxy-1-({4-[(2-oxo-1,2-dihydropyridin-1-yl)methyl]phenyl}methyl)-1H-pyrazole-4-carboxamide |
| Synonyms | KVD-900, K-VD-900, Sebetralstat; Sebetralstat free base; |
| Molecular Formula | C25H24FN5O4 |
| Molecular Weight | 477.49 |
| Smile | O=C(C1=CN(CC2=CC=C(CN3C=CC=CC3=O)C=C2)N=C1OC)NCC4=NC=CC(OC)=C4F |
| InChiKey | QTNIRGIZAWMZRE-UHFFFAOYSA-N |
| InChi | InChI=1S/C25H24FN5O4/c1-34-21-10-11-27-20(23(21)26)13-28-24(33)19-16-31(29-25(19)35-2)15-18-8-6-17(7-9-18)14-30-12-4-3-5-22(30)32/h3-12,16H,13-15H2,1-2H3,(H,28,33) |
| CAS Number | 1933514-13-6 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | Refer to MSDS |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code | 2934200090 |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Davie RL, Edwards HJ, Evans DM, Hodgson ST, Stocks MJ, Smith AJ, Rushbrooke LJ, Pethen SJ, Roe MB, Clark DE, McEwan PA, Hampton SL. Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema. J Med Chem. 2022 Oct 27;65(20):13629-13644. doi: 10.1021/acs.jmedchem.2c00921. Epub 2022 Oct 17. PMID: 36251573; PMCID: PMC9620001.
2: Mutch P, Bashir M, Jung B, Yi P, Iverson M. Absorption, metabolism, and excretion of [14C]-sebetralstat (KVD900) following a single oral dose in healthy male participants. Xenobiotica. 2022 Jul;52(7):707-717. doi: 10.1080/00498254.2022.2132187. Epub 2022 Oct 17. PMID: 36200371.
3: Duckworth EJ, Murugesan N, Li L, Rushbrooke LJ, Lee DK, De Donatis GM, Maetzel A, Yea CM, Hampton SL, Feener EP. Pharmacological suppression of the kallikrein kinin system with KVD900: An orally available plasma kallikrein inhibitor for the on-demand treatment of hereditary angioedema. Clin Exp Allergy. 2022 Sep;52(9):1059-1070. doi: 10.1111/cea.14122. Epub 2022 Mar 20. PMID: 35278245; PMCID: PMC9544254.
4: Maetzel A, Smith MD, Duckworth EJ, Hampton SL, De Donatis GM, Murugesan N, Rushbrooke LJ, Li L, Francombe D, Feener EP, Yea CM. KVD900, an oral on-demand treatment for hereditary angioedema: Phase 1 study results. J Allergy Clin Immunol. 2022 Jun;149(6):2034-2042. doi: 10.1016/j.jaci.2021.10.038. Epub 2022 Jan 24. PMID: 35086692.
Chemical Structure
