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Cat. No.: HY-118917

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VX-148

VX-148 is an orally active IMPDH inhibitor. VX-148 reversibly and non-competitively inhibits human IMPDH type I and type II at the NAD cofactor binding site (with K_i of 14 nM and 6 nM, respectively), blocks the de novo biosynthesis of guanine nucleotides, and selectively inhibits the proliferation of mitogen-stimulated lymphocytes. VX-148 inhibits the primary antibody response to sheep red blood cells in mice, prolongs skin graft survival in MHC-mismatched mouse models, and can be used for research on skin transplant rejection.

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CAS No.: 297730-05-3
Formule: C₂₃H₂₅N₅O₄
Masse moléculaire:435.48

Stockage:

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

Data Sheet (273 KB)

VX-148 Chemical Structure

CAS No.: 297730-05-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

IMPDH1

14 nM (Ki)

IMPDH2

6 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
L1210	IC50	309 nM	Antiproliferative activity against mouse L1210 lymphoid T cells assessed as viability reduction incubated 72 hrs by XTT assay. Antiproliferative activity against mouse L1210 lymphoid T cells assessed as viability reduction incubated 72 hrs by XTT assay.	12183689
Jurkat	IC50	245 nM	Antiproliferative activity against human Jurkat lymphoid T cells assessed as viability reduction incubated 72 hrs by XTT assay. Antiproliferative activity against human Jurkat lymphoid T cells assessed as viability reduction incubated 72 hrs by XTT assay.	12183689
Raji	IC50	279 nM	Antiproliferative activity against human Raji lymphoid B cells assessed as viability reduction incubated 72 hrs by XTT assay. Antiproliferative activity against human Raji lymphoid B cells assessed as viability reduction incubated 72 hrs by XTT assay.	12183689
U-937	IC50	511 nM	Antiproliferative activity against human U937 monocytes assessed as viability reduction incubated 72 hrs by XTT assay. Antiproliferative activity against human U937 monocytes assessed as viability reduction incubated 72 hrs by XTT assay.	12183689
WI-38	IC50	> 20000 nM	Antiproliferative activity against human WI38 fibroblasts assessed as viability reduction incubated 72 hrs by XTT assay. Antiproliferative activity against human WI38 fibroblasts assessed as viability reduction incubated 72 hrs by XTT assay.	12183689
Hs68	IC50	> 20000 nM	Antiproliferative activity against human Hs68 fibroblasts assessed as viability reduction incubated 72 hrs by XTT assay. Antiproliferative activity against human Hs68 fibroblasts assessed as viability reduction incubated 72 hrs by XTT assay.	12183689

In Vitro

Adaptive ImmunityNucleotide MetabolismCarbohydrate MetabolismOthers

Adaptive Immunity

VX-148 (20 μM-20 nM; 3-day experiment) inhibits the proliferation of mouse and rat T lymphocytes and B lymphocytes, with IC₅₀ values ranging from 83 to 302 nM^[1].

Adaptive Immunity

Nucleotide Metabolism

VX-148 (20 μM-20 nM; 3-day experiment) inhibits PHA-stimulated human PBMC T cells and SPAS-stimulated B cells with IC₅₀ values of 82 and 73 nM, respectively, and this effect is reversed by 50 μM guanosine^[1].

Carbohydrate Metabolism

VX-148 shows no inhibition of either NAD/NADPH dehydrogenase at concentrations up to 50 μM^[1].

Nucleotide Metabolism

VX-148 (10 min preincubation-10 min readout) is a noncompetitive inhibitor of recombinant human IMPDH type I and type II, with K_i values of 14 nM and 6 nM, respectively^[1].

Others

VX-148 (72 hours) inhibits the proliferation of L1210, Jurkat, Raji, and U937 with IC₅₀ values of 245-511 nM, but shows no inhibitory effect on WI38 or Hs68 fibroblasts at > 20,000 nM^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_0-t	AUC_inf	T_1/2	C_max	T_max
Mice^[1]	25 mg/kg	p.o.	6.5 μg·h/mL	6.69 μg·h/mL	3.42 h	3.32 μg/mL	0.5 h
Mice^[1]	50 mg/kg	p.o.	14.3 μg·h/mL	14.5 μg·h/mL	1.1 h	8.30 μg/mL	0.25 h
Mice^[1]	100 mg/kg	p.o.	45.8 μg·h/mL	48.3 μg·h/mL	1.81 h	22.0 μg/mL	0.5 h
Mice^[1]	100 mg/kg	p.o.	35.9 μg·h/mL	37.3 μg·h/mL	1.89 h	17.3 μg/mL	0.5 h

In Vivo

Adaptive ImmunityImmune Tolerance & Immunosuppression

Adaptive Immunity

VX-148 (25-100 mg/kg; p.o.; twice daily; Day 1 to Day 4) reduces SRBC-specific IgM plaque-forming cells in a dose-dependent manner in adult female CD-1 mice, with an ED₅₀ of 38 mg/kg^[1].

Adaptive Immunity

Immune Tolerance & Immunosuppression

VX-148 (25-100 mg/kg; p.o.; twice daily; for 11 days) prolongs the survival of BALB/c to C57BL/6 skin grafts, reaching 13.4 days at 100 mg/kg compared with 11.2 days in the vehicle group^[1].

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

Animal Model:

CD-1 (adult female)^[1]
Dosage:

25, 50, and 100 mg/kg
Administration:

p.o. (gavage); twice daily; day 1 through day 4
Result:

Reduced plaque formation by 25%, 66%, and 86% at 25, 50, and 100 mg/kg, respectively, relative to vehicle controls.
The ED₅₀ was 38 mg/kg, calculated from two independent PFC experiments.

Animal Model:

C57BL/6 (male recipient); BALB/c (donor)^[1]
Dosage:

25, 50, and 100 mg/kg
Administration:

p.o.; twice daily; for 11 days; first dose 30 min before transplant surgery
Result:

Prolonged the survival of BALB/c to C57BL/6 skin grafts, reaching 13.4 days at 100 mg/kg compared with 11.2 days in the vehicle group.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

Chemical Information

CAS No. 297730-05-3
Masse moléculaire 435.48
Formule C₂₃H₂₅N₅O₄
SMILES

O=C(O[C@@H](CC#N)CC)N[C@H](C1=CC=CC(NC(NC2=CC=C(C#N)C(OC)=C2)=O)=C1)C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 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)
Instruction de manipulation (2659 KB)

Références

[1]. Jain J, et al. Characterization of pharmacological efficacy of VX-148, a new, potent immunosuppressive inosine 5'-monophosphate dehydrogenase inhibitor. The Journal of pharmacology and experimental therapeutics. 2002 Sep;302(3):1272-7.

[2]. Shin WJ, et al. Identification of a Small Benzamide Inhibitor of Influenza Virus Using a Cell-Based Screening. Chemotherapy. 2016;61(3):159-66.

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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VX-148

Activité biologique

Description

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

VX-148 Related Classifications

HY-118917 Related Classifications

Bioz

Keywords

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