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Referencia número: HY-183409

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ONO-7684

Name: ONO-7684
Brand: MedChemExpress
SKU: HY-183409
Availability: PreOrder

(Synonyms: ONO-5450598)

ONO-7684 (ONO-5450598) is an orally active coagulation factor XIa (FXIa) inhibitor with a K_i value of 2 nM against human FXIa. ONO-7684 inhibits human FXIa in a competitive and reversible manner, reduces factor XI coagulation activity, prolongs activated partial thromboplastin time in a dose-dependent manner, and exerts no significant effects on PT/INR and the activity of related serine proteases. ONO-7684 exerts antithrombotic effects in vivo without prolonging bleeding time. ONO-7684 can be used in studies related to thromboembolic diseases.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 1941243-22-6
Fòrmula: C₂₃H₁₆ClF₂N₉O
Peso molecular:507.88

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

ONO-7684 Chemical Structure

No. CAS: 1941243-22-6

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- IC₅₀ & Target
- In Vitro
- Parmacokinetics
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Actividad biológica

Descripciòn

IC₅₀ & Target

^[2]

FXIa

2 nM (Ki, Human source FXIa)

In Vitro

ONO-7684 (ONO-5450598) potently and selectively inhibits activated human coagulation factor XIa with a K_i value of 2 nM, while it exhibits only extremely weak or no inhibitory activity against other tested human coagulation and fibrinolytic enzymes^[2].
ONO-7684 (0.46-0.8 μM) doubles APTT in human, monkey and rabbit plasma, but exerts no effect on PT at concentrations up to 33 μM^[2].
ONO-7684 exhibits detectable bidirectional permeability in human Caco-2 cells, with a flux of 2.5 × 10^-6 cm/sec in the A-to-B direction and 36 × 10^-6 cm/sec in the B-to-A direction^[2].
ONO-7684 exhibits detectable bidirectional permeability in the human colorectal cancer cell line Caco-2 within this experimental system, with a flux of 8.2 × 10^-6 cm/sec in the A→B direction and 28 × 10^-6 cm/sec in the B→A direction^[2].
ONO-7684 (0.5-1.2 μM) doubles the activated partial thromboplastin time (APTT) in human plasma^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_1/2	CL	Bioavailability
Dog^[2]	1 mg/kg	i.v.	3.6 h	2.8 mL/min/kg	/
Dog^[2]	1 mg/kg	p.o.	5.5 h	/	88 %
Monkey^[2]	1 mg/kg	i.v.	3.2 h	3.2 mL/min/kg	/
Monkey^[2]	1 mg/kg	p.o.	4.1 h	/	81 %

Chemical Information

No. CAS 1941243-22-6
Peso molecular 507.88
Fòrmula C₂₃H₁₆ClF₂N₉O
SMILES

O=C1N2[C@@H](C3=C(F)N=C(C4=C(N=C(C=C4)N)F)N3)CCC2=CC(C5=C(N6C=NN=N6)C=CC(Cl)=C5)=C1
Synonyms

ONO-5450598
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Beale D, et al. ONO-7684 a novel oral FXIa inhibitor: Safety, tolerability, pharmacokinetics and pharmacodynamics in a first-in-human study. British journal of clinical pharmacology. 2021 Aug;87(8):3177-3189. [Content Brief]

[2]. Kouyama S, et al. Discovery of ONO-5450598, a highly orally bioavailable small molecule factor XIa inhibitor: the pharmacokinetic and pharmacological profiles[J]. Res. Pract. Thromb. Haemost, 2017, 1(1): 1038.

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Calculadora de dilución

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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- In Vitro
Chemical Information
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ONO-7684