2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Tarafenacin

Tarafenacin (SVT-40776) is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin can be used in the research of overactive bladder.

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

Tarafenacin

Tarafenacin Chemical Structure

CAS No. : 385367-47-5

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Tarafenacin Related Antibodies

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Description

Tarafenacin (SVT-40776) is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin can be used in the research of overactive bladder[1][2][3].

IC50 & Target

mAChR3

0.19 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
0.9 nM
Compound: 4q
Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
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
Compound: 4q
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
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
Compound: 4q
Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
[PMID: 21524581]
In Vitro

Tarafenacin (3-1000 nmol/L; 60 min) potently inhibits carbachol-induced contractions in mouse isolated urinary bladder detrusor smooth muscle[1].
Tarafenacin (0.1-10 μmol/L; 60 min) inhibits Carbachol (HY-B1208)-induced negative chronotropism in mouse isolated atrial tissue, exhibiting a 199-fold functional selectivity for mouse urinary bladder over atrial tissue[1].
Tarafenacin (20 min) potently inhibits Carbachol-induced inositol phosphate accumulation in mouse bladder smooth muscle with a Ki of 0.19 nM, and shows 23-fold greater selectivity over mouse salivary glands[2].

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

Tarafenacin Related Antibodies
In Vivo

Tarafenacin (1-3000 nmol/kg (log dose); i.v.; cumulative bolus; 15 min between doses) potently inhibits spontaneous guinea pig bladder contractions with an ED25 of 6.97 mg/kg, and exhibits greater than 175-fold bladder versus vascular selectivity, with no observed effects on arterial blood pressure[1].

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

Animal Model: DH female guinea pigs (250-300 g)[1]
Dosage: 1-3000 nmol/kg (Log dose)
Administration: i.v.; cumulative bolus; 15 min between doses
Result: Inhibited spontaneous bladder contractions in a dose-dependent manner, with an ED25 of 17.1 nmol/kg.
Did not affect arterial blood pressure at tested doses, resulting in a bladder versus vascular selectivity of more than 175-fold.
Clinical Trial
Molecular Weight

408.39

Formula

C21H20F4N2O2
CAS No.
SMILES

O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4
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
References
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Tarafenacin Related Classifications

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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:

Tarafenacin385367-47-5SVT-40776SVT40776SVT 40776mAChRMuscarinic acetylcholine receptorM3 muscarinic receptordetrusor contractile activitybladder smooth muscleM2 muscarinic receptorsinositol phosphate accumulationoveractive bladder syndromeurinary tissuehuman M5 mAChRsalivary gland M3 receptorscardiac tissueInhibitorinhibitorinhibit

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