Synonym
BNC375; BNC-375; BNC 375;
IUPAC/Chemical Name
4-((1R,3R)-3-(((5-chloro-2-methoxyphenyl)amino)methyl)-2,2-dimethylcyclopropyl)benzenesulfonamide
InChi Key
LWWDCTBUJUEFDE-CRAIPNDOSA-N
InChi Code
InChI=1S/C19H23ClN2O3S/c1-19(2)15(11-22-16-10-13(20)6-9-17(16)25-3)18(19)12-4-7-14(8-5-12)26(21,23)24/h4-10,15,18,22H,11H2,1-3H3,(H2,21,23,24)/t15-,18-/m1/s1
SMILES Code
O=S(C1=CC=C([C@H]2C(C)(C)[C@@H]2CNC3=CC(Cl)=CC=C3OC)C=C1)(N)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Positive allosteric modulators (PAMs) of α7 nAChRs can have different properties with respect to their effects on channel kinetics. Type I PAMs amplify peak
channel response to acetylcholine but do not appear to influence channel desensitization kinetics, whereas Type II PAMs both increase channel response and delay receptor desensitization.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
394.91
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs
Andrew J. Harvey, Thomas D. Avery, Laurent Schaeffer, Christophe Joseph, Belinda C. Huff, Rajinder Singh, Christophe Morice, Bruno Giethlen, Anton A. Grishin, Carolyn J. Coles, Peter Kolesik, Stéphanie Wagner, Emile Andriambeloson, Bertrand Huyard, Etienne Poiraud, Dharam Paul, and Susan M. O’Connor
Publication Date (Web): March 25, 2019 (Letter)
DOI: 10.1021/acsmedchemlett.9b00001
