BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with IC50 of 506 nM and KD of 83.5 nM. BMPR2-IN-1 can be used in the research of pulmonary hypertension, Alzheimer's disease and cancer.

Physicochemical Properties

Molecular Formula	C18H16F3N7O3
Molecular Weight	435.36
Appearance	Solid powder
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). This product requires protection from light (avoid light exposure) during transportation and storage.(2). 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

References

[1]. Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2. ACS Med Chem Lett. 2023 May 30;14(6):833-840.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (229.69 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 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. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make up to 1 mL. *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.74 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, add 100 μL of 25.0 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: ≥ 2.5 mg/mL (5.74 mM)(saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. Take μL of DMSO stock solution and add μL. μL, mix well until clear, add μL Tween 80, mix well until clear, and add μL normal saline. Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear and transparent normal saline solution. If the continuous administration period exceeds half a month, please choose this solution with caution. Please ensure that the first step stock solution is dissolved to a clear state, and add co-solvents from left to right. You can use ultrasonic heating (ultrasonic cleaning instrument, recommended frequency 20-40 kHz), vortex blowing and other methods to assist dissolution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2969 mL	11.4847 mL	22.9695 mL
	5 mM	0.4594 mL	2.2969 mL	4.5939 mL
	10 mM	0.2297 mL	1.1485 mL	2.2969 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.