Description
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.
Product information
CAS Number: 1839519-57-1
Molecular Weight: 339.25
Formula: C14H15BrN2OS
Chemical Name: 7-bromo-N-[(3R)-piperidin-3-yl]-1-benzothiophene-2-carboxamide
Smiles: O=C(N[C@H]1CNCCC1)C1=CC2=CC=CC(Br)=C2S1
InChiKey: LRYYPTVUWGMZQB-SNVBAGLBSA-N
InChi: InChI=1S/C14H15BrN2OS/c15-11-5-1-3-9-7-12(19-13(9)11)14(18)17-10-4-2-6-16-8-10/h1,3,5,7,10,16H,2,4,6,8H2,(H,17,18)/t10-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Br-PBTC (0.01~10 μM; HEK cells) selectively affects 2 and 4 subunits. Br-PBTC (3 μM; oocytes) has greater effects on nAChRs with 2 subunits over those with 4 subunits. Br-PBTC (0.01~10 μM; 15 minutes; HEK cells) can increase channel activation by a maximal concentration of ACh. Br-PBTC (3 μM; 50 seconds; oocytes) increased ACh activation of α4β2 nAChRs by 385± 61 %. Br-PBTC (3 μM;oocytes) reactivates short term desensitized nAChRs expressed. Br-PBTC (3 μM; 500 seconds; HEK cells) reactivates short term desensitized (α4β2)2α4 and(α4β2)2β2 nAChRs expressed. Br-PBTC (0.1~100 μM;0~140 seconds; HEK cells) reactivates long term desensitized nAChRs.
Products are for research use only. Not for human use.
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