PeptideDB

BPAM344 1204572-55-3

BPAM344 1204572-55-3

CAS No.: 1204572-55-3

BPAM344 is a positive allosteric modulator (PAM) of the kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a.
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BPAM344 is a positive allosteric modulator (PAM) of the kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a.

Physicochemical Properties


Molecular Formula C10H11FN2O2S
Molecular Weight 242.27
Exact Mass 242.052
CAS # 1204572-55-3
PubChem CID 67531324
Appearance White to off-white solid powder
Density 1.5±0.1 g/cm3
Boiling Point 415.9±55.0 °C at 760 mmHg
Flash Point 205.3±31.5 °C
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.635
LogP 0.69
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 1
Heavy Atom Count 16
Complexity 377
Defined Atom Stereocenter Count 0
InChi Key FLTMTBPCYAZIKM-UHFFFAOYSA-N
InChi Code

InChI=1S/C10H11FN2O2S/c11-7-1-4-9-10(5-7)16(14,15)12-6-13(9)8-2-3-8/h1,4-5,8,12H,2-3,6H2
Chemical Name

4-cyclopropyl-7-fluoro-2,3-dihydro-1λ6,2,4-benzothiadiazine 1,1-dioxide
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: This product requires protection from light (avoid light exposure) during transportation and storage.
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 At the highest concentration measured (200 μM), BPAM344 potentiates glutamate-evoked currents of GluK2a 21-fold, with an EC50 of 79 μM. While BPAM344 only slightly affects deactivation kinetics, it significantly reduces desensitization kinetics (from 5.5 to 775 ms)[1]. Additionally, the AMPA receptor subunit GluA1i (5-fold) and the KAR subunits GluK3a (59-fold), GluK2a (15-fold), and GluK1b (5-fold) had their peak current amplitudes potentiated by BPAM344 (100 μM)[1].
References

[1]. Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors. Mol Pharmacol. 2017 Jun;91(6):576-585.


Solubility Data


Solubility (In Vitro) DMSO: 250 mg/mL (1031.91 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.08 mg/mL (8.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume 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: ≥ 2.08 mg/mL (8.59 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 20.8 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 3: ≥ 2.08 mg/mL (8.59 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 20.8 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 4.1276 mL 20.6381 mL 41.2763 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 mL
10 mM 0.4128 mL 2.0638 mL 4.1276 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.