[CAS NO. 2414674-71-6] SUVN-911
PRODUCTS SPECIFICATIONS [2414674-71-6]
DESCRIPTION [2414674-71-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 261.15 |
| Molecular Formula | C11H14Cl2N2O |
| SMILES | ClC1=NC=C(OC[C@H]2N[C@@H]3C[C@@H]3C2)C=C1.[H]Cl |
Summary
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a K i of 1.5 nM. SUVN-911 has antidepressant activity [1] .
IC50 & Target
Ki: 1.5 nM (α4β2 receptor) [1]
In Vitro
SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR
[1]
.
SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SUVN-911 is devoid of cardiovascular and gastrointestinal side effects
[1]
.
SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects
[1]
.
SUVN-911 shows metabolic stability in rats
[1]
.
SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Wistar rats (180-230 g) [1] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10.0 mg/kg |
| Administration: | Oral administration, daily, for 3 days |
| Result: | Showed antidepressant like activity with no signs of tachyphylaxis. |
| Animal Model: | Male Wistar rats (225 ± 25 g) [1] |
| Dosage: | 3 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Oral administration |
| Result: | AUC=3507 ng*h/mL, T 1/2 =3.34 hours. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03551288 | Suven Life Sciences Limited |
Major Depressive Disorder
|
May 22, 2018 | Phase 1 |
| NCT03155503 | Suven Life Sciences Limited |
Depressive Disorder, Major
|
May 22, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 125 mg/mL ( 478.65 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.8292 mL | 19.1461 mL | 38.2922 mL |
| 5 mM | 0.7658 mL | 3.8292 mL | 7.6584 mL |
| 10 mM | 0.3829 mL | 1.9146 mL | 3.8292 mL |