Fig. 1 · Structure

Cat. No.: A10808
CAS No.: 385367-47-5
Formula: C₂₁H₂₀F₄N₂O₂
Mol. Weight: 408.39

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Tarafenacin (SVT-40776)

Name: Tarafenacin (SVT-40776)
Brand: Adooq Bioscience
SKU: A10808
Availability: InStock

Cat. No. A10808 CAS 385367-47-5

muscarinic receptor antagonist

SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder.

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Biological Activity

Cellular Effect

Cell Line	Activity	Value	Description	Reference
CHO-K1	IC50	0.9 nM	Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]
CHO-K1	IC50	1.5 nM	Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]
CHO-K1	IC50	97.3 nM	Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]

In Vitro Studies

Tarafenacin was evaluated in recombinant supersomes using incubations with and without the compound. The IC50 value determined with CYP2C9 supersomes was >100 μM. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Tarafenacin evaluation in recombinant supersomes

Biochemical assay · recombinant supersomes [1]

Recombinant supersomes were incubated with and without Tarafenacin. The IC50 value determined with CYP2C9 supersomes was >100 μM.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
IC50 values determined with CYP2C9 supersomes	IC50 >100 μM	[1]

Literature-Reported Treatment Conditions

Treatment concentration: 0.3, 1, 3, 10, 20, 30, 50, 60, 70, 90 and 100 μM
Exposure duration: started after 6 min of preincubation by adding NADPH and terminated after 15 min
Method: incubated with and without the study compounds
Vehicle: DMSO

Methods and source locations

Compound reported in the paper: Tarafenacin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Experimental materials and methods > Chemical and reagents (S38); Experimental materials and methods > Inhibition of CYP2C9 on recombinant supersomes and calculation of IC50 (S66, S67, S68, S70, S73); Table 5 (T5.h1, T5.r14)

IC50 values determined with CYP2C9 supersomes: IC50 values determined with CYP2C9 supersomes; comparator: solvent control = 100% — Table 5 (T5.h1, T5.r14)

Specifications

Manufacturer	Adooq Bioscience
Actions	Antagonist
CAS Number	385367-47-5
Applications	muscarinic receptor antagonist
Formula	C₂₁H₂₀F₄N₂O₂
Molecular Weight	408.39
Synonyms	SVT40776
SMILES	C1CN2CCC1[C@H](C2)OC(=O)N(CC3=CC(=C(C(=C3)F)F)F)C4=CC(=CC=C4)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Goldwaser E, Laurent C, Lagarde N, et al. Machine learning-driven identification of drugs inhibiting cytochrome P450 2C9. PLoS Comput Biol (2022). PMID: 35081108 DOI: 10.1371/journal.pcbi.1009820 Source material