EVT-401

Cat. No.: HY-178230: Data Sheet Handling Instructions
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EVT-401 is an orally active, potent and highly selective human P2X7R antagonist, with an IC₅₀ of 10 nM and a K_i of 7.6 nM for human P2X7R, and an IC₅₀ of 220 nM for mouse P2X7R. EVT-401 promotes apoptosis and induces cell cycle arrest in human rheumatoid arthritis synovial fibroblasts (RA SF), reduces the production of proinflammatory and joint-destructive mediators, and mitigates aggressive phenotypes. EVT-401 exhibits favorable oral bioavailability and a good safety profile, making it suitable for research into rheumatoid arthritis.

For research use only. We do not sell to patients.

EVT-401 Chemical Structure

CAS No. : 951015-69-3

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Other Forms of EVT-401:

(Rac)-EVT-401 In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

hP2X7R

10 nM (IC₅₀)

hP2X7R

7.6 nM (Ki)

rP2X7R

220 nM (IC₅₀)

In Vitro

EVT-401 binds to hP2X7R with a K_i of 7.6 nM in radioligand binding assays, and Schild analysis yields a K_B of 12.1 nM^[1].
EVT-401 inhibits hP2X7R-mediated calcium influx with an IC₅₀ of 10 nM in calcium flux assays using 1321N1 cells, whereas its IC₅₀ for rat P2X7R is 220 nM, and it shows no significant inhibition of P2X1/2/3/4 family members^[1].
EVT-401 (10-200 μM; 24-96 h) exhibits low cytotoxicity in RA SF ^[1].
EVT-401 (50-200 μM; 24 or 48 h) promotes apoptosis in RA SF as determined by Annexin V/7-AAD flow cytometry^[1].
EVT-401 (100 μM; 24 h) induces G0/G1 cell cycle arrest in RA SF and reduces the levels of G0/G1-related proteins including Cdk2, Rb and p-Rb^[1].
EVT-401 (100 μM; 24 h) significantly reduces IL-6 secretion and downregulates MMP-3 and DKK-1 expression in a TNF-α-induced RA SF inflammatory model^[1].
EVT-401 (10 or 100 μM; 24 h) inhibits the migration and invasion of RA SF in Transwell and wound healing assays^[1].

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

Cell Viability Assay

Cell Line:	RA SF
Concentration:	10, 50, 100 and 200 μM
Incubation Time:	24, 48, 72 and 96 h
Result:	Showed low cytotoxicity in RA SF.

Cell Proliferation Assay

Cell Line:	RA SF
Concentration:	10, 50, 100 and 200 μM
Incubation Time:	24, 48, 72 and 96 h
Result:	At 100 μM partially inhibited RA SF proliferation after 72 h, while concentrations below 100 μM showed no obvious antiproliferative effects within 24, 48 or 72 h.

Apoptosis Analysis

Cell Line:	RA SF
Concentration:	50, 100 and 200 μM
Incubation Time:	24 or 48 h
Result:	Promoted apoptosis in RA SF, as detected by Annexin V/7-AAD flow cytometry. The pro-apoptotic effect was more obvious.

Cell Cycle Analysis

Cell Line:	RA SF
Concentration:	50, 100 and 200 μM
Incubation Time:	24 h
Result:	Induced G0/G1 cell cycle arrest in RA SF.

Cell Migration Assay

Cell Line:	TNF-α-stimulated RA SF
Concentration:	10 and 100 μM
Incubation Time:	24 h
Result:	Suppressed TNF-α-induced transwell migration of RA SF.

Cell Invasion Assay

Cell Line:	TNF-α-stimulated RA SF
Concentration:	10 and 100 μM
Incubation Time:	24 h
Result:	Inhibited the invasive potential of RA SF through Matrigel-coated transwell membranes.

Western Blot Analysis

Cell Line:	RA SF
Concentration:	10 and 100 μM
Incubation Time:	24 h
Result:	Reduced the levels of G0/G1 phase-related proteins, including Cdk2, Rb and p-Rb, in RA SF.

Parmacokinetics

Species	Dose	Route	AUC_0-t	MRT_0-t	T_1/2	T_max	CL_z/F	V_z/F	C_max
Cynomolgus Monkey^[1]	10 mg/kg	p.o.	5407.69 μg/L·h	11.65 h	10.56 h	3 h	1.76 L/h/kg	26.39 L/kg	403.51 μg/L
Cynomolgus Monkey^[1]	100 mg/kg	p.o.	34246.4 μg/L·h	12.61 h	9.87 h	5.67 h	3.15 L/h/kg	45.94 L/kg	2457.04 μg/L
Cynomolgus Monkey^[1]	30 mg/kg	p.o.	11940.18 μg/L·h	13.49 h	12.86 h	2.29 h	2.46 L/h/kg	42.66 L/kg	891.24 μg/L

In Vivo

EVT-401 (0.5, 5 and 50 mg/kg; p.o.; once daily; for 28 days) shows detectable differences in plasma concentrations in female Lewis rat collagen-induced arthritis models^[1].
EVT-401 (100 mg/kg; p.o.; once daily; for 8 weeks) significantly reduces clinical arthritis scores, shows a decreasing trend in serum CRP levels, and does not cause obvious pathological damage in the heart, liver, spleen, lung or kidney as assessed by H&E staining in cynomolgus monkey collagen-induced arthritis models^[1].
EVT-401 (100 μM; s.c.; twice weekly; for 21 days) significantly inhibits RA SF invasion into cartilage in RA SF-cartilage co-transplantation NOD-SCID mouse models^[1].
EVT-401 shows dose-dependent oral bioavailability of 42.2%, 30.9% and 26.6% at doses of 10, 30 and 100 mg/kg, respectively, in cynomolgus monkeys^[1].

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

Animal Model:	Female Lewis rats with collagen-induced arthritis^[1]
Dosage:	0.5, 5, and 50 mg/kg
Administration:	Oral gavage (p.o.); once daily; for 28 days
Result:	Showed detectable differences in plasma concentrations. Did not exhibit significant therapeutic effects in this arthritis model.

Animal Model:	Cynomolgus monkeys with collagen-induced arthritis^[1]
Dosage:	100 mg/kg
Administration:	Oral gavage (p.o.); once daily; for 8 weeks
Result:	Significantly reduced clinical arthritis scores. Showed a decreasing trend in serum CRP levels. Did not cause obvious pathological damage in heart, liver, spleen, lung, or kidney by H&E staining.

Animal Model:	NOD-SCID mice with RA SF-cartilage co-transplantation^[1]
Dosage:	100 μM
Administration:	Subcutaneous injection (s.c.); twice weekly; for 21 days
Result:	Significantly inhibited RA SF invasion into cartilage.

Molecular Weight

436.40

Formula

C₂₂H₂₀F₄N₂O₃

CAS No.

951015-69-3

SMILES

FC(C=C1CC(NC2=C3C(C(N(C=C3)[C@H](C)CO)=O)=CC=C2C)=O)=C(C=C1)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Rao P et al. P2X7R of synovial fibroblasts is a potential therapeutic target associated with refractory rheumatoid arthritis. Sci Adv. 2026 May 22;12(21):eadw9543.

EVT-401 Related Classifications

Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EVT-401951015-69-3EVT401EVT 401P2X ReceptorApoptosisP2XRsP2X7R inhibitorRheumatoid arthritisnonobese diabetic mice (NOD)–severe combined immunodeficient (SCID) miceSynovial fibroblasts (SF)Inhibitorinhibitorinhibit

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