Cart
sales@molnova.com
Darexaban
CAS No. 365462-23-3
Darexaban( YM150 | YM-150 | YM 150 )
Catalog No. M14257 CAS No. 365462-23-3
A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 51 | In Stock |
|
| 5MG | 78 | In Stock |
|
| 10MG | 132 | In Stock |
|
| 25MG | 266 | In Stock |
|
| 50MG | 434 | In Stock |
|
| 100MG | 620 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
| 1 mL x 10 mM in DMSO | 88 | In Stock |
|
| 5MG | 83 | In Stock |
|
| 10MG | 140 | In Stock |
|
| 25MG | 235 | In Stock |
|
| 50MG | 346 | In Stock |
|
| 100MG | 500 | In Stock |
|
| 200MG | 712 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameDarexaban
-
NoteResearch use only, not for human use.
-
Brief DescriptionA potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM.
-
DescriptionA potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM; displays high selectivities over other related serine proteases, such as trypsin, thrombin and kallikrein (IC50>10 uM); demonstrates potent anticoagulant activities both in vitro and in vivo, shows potential for prevention and treatment of thromboembolic diseases.Thrombosis Phase 2 Discontinued.
-
In VitroDarexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa.
-
In VivoIn mice, Darexaban inhibits FXa activity in plasma with an ED50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg. In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg.In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher.
-
SynonymsYM150 | YM-150 | YM 150
-
PathwayMetabolic Enzyme/Protease
-
TargetFactor Xa
-
RecptorFactor Xa
-
Research AreaCardiovascular Disease
-
IndicationThrombosis
Chemical Information
-
CAS Number365462-23-3
-
Formula Weight474.561
-
Molecular FormulaC27H30N4O4
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 250 mg/mL (526.81 mM)
-
SMILESO=C(NC1=C(NC(C2=CC=C(OC)C=C2)=O)C=CC=C1O)C3=CC=C(N4CCN(C)CCC4)C=C3
-
Chemical NameN-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Hirayama F, et al. J Med Chem. 2011 Dec 8;54(23):8051-65.
2. Iwatsuki Y, Eur J Pharmacol. 2011 Dec 30;673(1-3):49-55.
3. Funatsu T, et al. J Thromb Haemost. 2012 Apr;10(4):703-5.
4. Steg PG, et al. Eur Heart J. 2011 Oct;32(20):2541-54.
molnova catalog
related products
-
Letaxaban
Letaxaban (TAK-442, TAK442) is a potent, selective and direct factor Xa (FXa) inhibitor with Ki of 1.8 nM for hFXa.
-
Edoxaban (b)
A potent and orally active Factor Xa inhibitor with Ki of 0.561 nM.
-
5-R-Rivaroxaban
5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor (IC50 0.7 nM; Ki 0.4 nM).
