Alogabat free base
Alogabat is a positive allosteric modulator and agonist of the GABAA α5 receptor.
For research use only. Not for human or veterinary use.
Alogabat structure
CAS No.: 2230009-48-8
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 698.00 | BP-00042-100mg | In stock | Get quote |
| 250 mg | USD 1,198.00 | BP-00042-250mg | In stock | Get quote |
| 500 mg | USD 1,988.00 | BP-00042-500mg | In stock | Get quote |
| 1 g | USD 2,580.00 | BP-00042-1g | In stock | Get quote |
| 2 g | Inquire | BP-00042-2g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction.
Biological activity
In Vitro Alogabat (compound 8) binds selectively to the α5 subunit over α1, α2, and α3. The Ki in HEK293 cells is 8.7 nM (hGABA-Aα5β3γ2). Alogabat (30×Ki=261 nM, transient) potently enhances GABA-evoked currents in oocytes with an efficiency of 97% to elicit 20% of the maximal current response (EC20).
Identifiers
- SMILES
-
O=C(NC1CCOCC1)C2=NN=C(OCC=3C(=NOC3C)C=4C=NC(=CC4)C)C=C2 - InChIKey
-
ACZCJTHHWMBFKC-UHFFFAOYSA-N
Specifications
- MW (average)
- 409.4384
- Formula
- C21H23N5O4
- CAS No.
- 2230009-48-8
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- 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
- Powder -20°C, 3 years , 4°C, 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
- In vitro
- DMSO : 33.33 mg/mL