Tarafenacin D-tartrate (Synonyms: SVT-40776 D-tartrate)

Cat. No.: HY-14825A Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

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Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.

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

Tarafenacin D-tartrate Chemical Structure

CAS No. : 1159101-48-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 451	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 451	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 264	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 410	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1080	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1836	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of Tarafenacin D-tartrate:

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Description

Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor. IC50 value: 0.19 nM (Ki) [1] Target: M3 muscarinic receptor in vitro: SVT-40776 is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 was the most potent in inhibiting carbachol-induced bladder contractions of the anti-cholinergic agents tested, without affecting atrial contractions over the same range of concentrations. SVT-40776 exhibited the highest urinary versus cardiac selectivity (199-fold) [1]. SVT-40776 has a much higher binding affinity (K(d) = 0.4 nM) to M5 mAChR than that of solifenacin (K(d) = 31 nM) with the same reeptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to SVT-40776 is in good agreement with the experimentally derived binding free energy change (-2.58 kcal/mol), suggesting that our modeled M5 mAChR structure and its complexes with the antagonists are reliable [2]. in vivo: In the guinea pig in vivo model, SVT-40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v), without affecting arterial blood pressure [1].

IC₅₀ & Target

mAChR3

Clinical Trial

Molecular Weight

558.48

Formula

C₂₅H₂₆F₄N₂O₈

CAS No.

1159101-48-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4.O[C@@H]([C@@H](C(O)=O)O)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (179.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7906 mL	8.9529 mL	17.9057 mL
5 mM	0.3581 mL	1.7906 mL	3.5811 mL
10 mM	0.1791 mL	0.8953 mL	1.7906 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (258 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. Salcedo C, et al. In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. Br J Pharmacol. 2009 Mar;156(5):807-17. [Content Brief]

[2]. Huang X, et al. Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation. J Phys Chem B. 2012 Jan 12;116(1):532-41. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7906 mL	8.9529 mL	17.9057 mL	44.7644 mL
	5 mM	0.3581 mL	1.7906 mL	3.5811 mL	8.9529 mL
	10 mM	0.1791 mL	0.8953 mL	1.7906 mL	4.4764 mL
	15 mM	0.1194 mL	0.5969 mL	1.1937 mL	2.9843 mL
	20 mM	0.0895 mL	0.4476 mL	0.8953 mL	2.2382 mL
	25 mM	0.0716 mL	0.3581 mL	0.7162 mL	1.7906 mL
	30 mM	0.0597 mL	0.2984 mL	0.5969 mL	1.4921 mL
	40 mM	0.0448 mL	0.2238 mL	0.4476 mL	1.1191 mL
	50 mM	0.0358 mL	0.1791 mL	0.3581 mL	0.8953 mL
	60 mM	0.0298 mL	0.1492 mL	0.2984 mL	0.7461 mL
	80 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5596 mL
	100 mM	0.0179 mL	0.0895 mL	0.1791 mL	0.4476 mL

Tarafenacin D-tartrate Related Classifications

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:

Tarafenacin1159101-48-0SVT-40776SVT40776SVT 40776mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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