| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
VA-K-14 hydrochloride targets the thyroid-stimulating hormone receptor (TSHR), a G protein-coupled receptor that is expressed on thyroid follicular cells and plays a critical role in regulating thyroid hormone production and thyroid gland growth. TSHR is the primary target of autoantibodies in Graves' disease, a condition characterized by hyperthyroidism caused by TSHR-stimulating antibodies. VA-K-14 HCl acts as a selective TSHR antagonist, binding to the receptor and inhibiting its activation by TSH and TSHR-stimulating antibodies. The compound has an IC50 of 12.3 μM. By blocking TSHR signaling, VA-K-14 HCl abrogates the downstream effects of TSHR activation, including cAMP production and thyroid hormone synthesis.
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| ln Vitro |
In vitro, VA-K-14 hydrochloride is a selective TSHR antagonist with an IC50 of 12.3 μM. It inhibits TSHR stimulation by serum and monoclonal TSHR-stimulating antibodies from patients with Graves' disease. The compound abrogates TSHR signaling. Its potency and selectivity for TSHR over other receptors have been characterized in cell-based assays using cells expressing TSHR.
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| ln Vivo |
In vivo, VA-K-14 hydrochloride has potential applications in the study of Graves' disease and other TSHR-mediated conditions. By blocking TSHR signaling, the compound may have therapeutic potential for hyperthyroidism and other disorders caused by TSHR activation. However, detailed in vivo efficacy data are limited.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for VA-K-14 hydrochloride involve measuring its binding affinity to the thyroid-stimulating hormone receptor (TSHR). Radioligand binding assays using membrane preparations from cells expressing TSHR are performed with a radiolabeled TSHR ligand (e.g., [¹²⁵I]-TSH) and varying concentrations of VA-K-14 HCl. Binding affinity (IC50 or Ki) is determined by competitive displacement.
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| Cell Assay |
In vitro cell-based experiments for VA-K-14 hydrochloride are conducted using cells expressing TSHR. Cells are treated with VA-K-14 HCl at varying concentrations and stimulated with TSH or TSHR-stimulating antibodies. cAMP accumulation is measured to assess TSHR signaling inhibition. The compound's ability to inhibit TSHR stimulation is quantified, and IC50 values are calculated from inhibition curves.
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| Animal Protocol |
In vivo animal experiments for VA-K-14 hydrochloride are performed in animal models of Graves' disease or other TSHR-mediated conditions. The compound is administered, and thyroid hormone levels, TSHR signaling, and disease severity are assessed. However, detailed in vivo efficacy data are limited.
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| ADME/Pharmacokinetics |
VA-K-14 hydrochloride is a small molecule (MW 341.86, formula C18H16ClN3S) with suitable physicochemical properties for research use. The compound is soluble in DMSO (50 mg/mL). Detailed pharmacokinetic parameters are limited in available literature.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for VA-K-14 hydrochloride are limited. The compound is supplied for laboratory research use only. As a TSHR antagonist, potential effects on thyroid function and hormone homeostasis should be considered.
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| References | |
| Additional Infomation |
VA-K-14 hydrochloride is also known as VAK14 HCl and VA-K-14 HCl. It is a research compound used primarily for studying the role of TSHR in thyroid function and for exploring new therapeutic strategies for Graves' disease and other TSHR-mediated conditions. Its selectivity for TSHR makes it a valuable tool for dissecting TSHR signaling pathways. The compound is not approved for clinical use.
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| Molecular Formula |
C18H16CLN3S
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|---|---|
| Molecular Weight |
341.857741355896
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| Exact Mass |
305.098
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| CAS # |
1171341-19-7
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| Related CAS # |
1013553-94-0;1171341-19-7 (HCl);
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| PubChem CID |
17479126
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| Appearance |
Off-white to gray solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
510.1±52.0 °C at 760 mmHg
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| Flash Point |
262.3±30.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.732
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| LogP |
4.33
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MMEANJJDNROSBC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15N3S.ClH/c1-19-18-21-15(11-22-18)16-13-9-5-6-10-14(13)20-17(16)12-7-3-2-4-8-12/h2-11,20H,1H3,(H,19,21)1H
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| Chemical Name |
N-Methyl-4-(2-phenyl-1H-indol-3-yl)-thiazole-2-amine Hydrochloride
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| Synonyms |
VA-K-14 Hydrochloride VA K 14 Hydrochloride VA-K-14 HCl VA K 14 HCl VAK14 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~146.26 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9252 mL | 14.6259 mL | 29.2517 mL | |
| 5 mM | 0.5850 mL | 2.9252 mL | 5.8503 mL | |
| 10 mM | 0.2925 mL | 1.4626 mL | 2.9252 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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