PeptideDB

MT-1207 1610794-70-1

MT-1207 1610794-70-1

CAS No.: 1610794-70-1

MT-1207 is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. The IC50 of MT-1207 for α1A, α1B
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MT-1207 is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. The IC50 of MT-1207 for α1A, α1B, α1D and 5-HT2A are <0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM, respectively. MT-1207 effectively lowers blood pressure (BP) in the 2K2C rat model without impairing renal function. MT-1207 is a multi-target inhibitor with the potential for vasodilation studies.

Physicochemical Properties


Molecular Formula C21H25CLN6S
Molecular Weight 428.98
CAS # 1610794-70-1
Appearance Typically exists as solids at room temperature
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets α1A-adrenergic receptor 0.1 nM (IC50) α1B-adrenergic receptor 0.15 nM (IC50) α1B-adrenergic receptor 1.40 nM (Ki) α1D-adrenergic receptor 0.086 nM (IC50) α1D-adrenergic receptor 0.69 nM (Ki) 5-HT2A Receptor 0.27 nM (IC50) 5-HT2A Receptor 0.079 nM (Ki)
References

[1]. Peng Wang, et al. Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension. J Med Chem. 2024 Jul 5.


Solubility Data


Solubility (In Vitro) DMSO : ~100 mg/mL (~233.11 mM; with ultrasonication)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 5 mg/mL (11.66 mM) (saturation unknown) in 10% DMSO +40% PEG300 +5% Tween-80 +45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution。
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 5 mg/mL (11.66 mM) (saturation unknown) in 10% DMSO +90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution。
For example, if 1 mL of working solution is to be prepared, You can add 100 μL of the 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 3: ≥ 5 mg/mL (11.66 mM) (saturation unknown) in 10% DMSO +90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),
For example, if 1 mL of working solution is to be prepared, you can add10% DMSO +90% Corn Oil


For example, if 1 mL of working solution is to be prepared, You can add 100 μL of the 50.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well.

" (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3311 mL 11.6556 mL 23.3111 mL
5 mM 0.4662 mL 2.3311 mL 4.6622 mL
10 mM 0.2331 mL 1.1656 mL 2.3311 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.