BTD is a novel selective activator of TRPC5 (Transient Receptor Potential Cation Channel Subfamily C Member 5). TRPC5 channel is a nonselective cation channel that participates in diverse physiological processes. TRPC5 inhibitors show promise in the treatment of anxiety.

Physicochemical Properties

Molecular Formula	C24H33N3O4S
Molecular Weight	459.601525068283
Exact Mass	459.219
CAS #	896684-04-1
PubChem CID	46369355
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Index of Refraction	1.691
LogP	2.63
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	8
Heavy Atom Count	32
Complexity	809
Defined Atom Stereocenter Count	0
InChi Key	YXADKMPRWFBOHW-UHFFFAOYSA-N
InChi Code	InChI=1S/C24H33N3O4S/c1-16-3-4-21-20(9-16)26-22(27-32(21,29)30)5-6-23(28)25-7-2-8-31-24-13-17-10-18(14-24)12-19(11-17)15-24/h3-4,9,17-19H,2,5-8,10-15H2,1H3,(H,25,28)(H,26,27)
Chemical Name	N-[3-(1-adamantyloxy)propyl]-3-(6-methyl-1,1-dioxo-4H-1λ6,2,4-benzothiadiazin-3-yl)propanamide
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
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

ln Vitro	With EC50 values of 1.4 μM in the fluorescent microwell Ca2+ test and 1.3 μM in whole-cell patch clamp assays, BTD can activate TRPC5 [1]. With an EC50 value of 20.6 μM, BTD can activate HEK293 cells expressing TRPM8 [1]. BTD can also activate a heteromeric channel complex made up of TRPC5, TRPC1, and TRPC4, which are near cousins of TRPC5.
References	[1]. A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels. Cell Calcium. 2017;66:10-18.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~217.58 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.44 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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 2: ≥ 2.5 mg/mL (5.44 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 is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1758 mL	10.8790 mL	21.7581 mL
	5 mM	0.4352 mL	2.1758 mL	4.3516 mL
	10 mM	0.2176 mL	1.0879 mL	2.1758 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.