| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Saredutant (SR-48968; SR-48968C) is a potent and selective NK2 receptor antagonist potentially for the treatment of major depressive disorder. Saredutant has both antidepressant-like effects and synergizes with desipramine in an animal model of depression. Saredutant, ameliorates stress-induced conditions without impairing cognition. SR 48968 specifically depresses neurokinin A- vs. substance P-induced hyperalgesia in a nociceptive withdrawal reflex. SR 48968 inhibits citric acid-induced airway hyperresponsiveness in guinea pigs.
| ln Vivo |
In animal models of depression, serodutant, an NK2 receptor antagonist, has synergistic effects with desipramine and antidepressant-like effects. The effect of saredutant on immobility during swimming tests varies with dose; immobility is not affected at low doses of 1 mg/kg, but is dramatically reduced at doses of 3 and 10 mg/kg [1].
|
|---|---|
| References | |
| Additional Infomation |
Saredutant (SR 48968) is a neurokinin-2 antagonist drug being developed as an antidepressant and anxiolytic by Sanofi-Aventis.
Drug Indication Investigated for use/treatment in depression and anxiety disorders. Mechanism of Action Saredutant works by blocking the effects of Neurokinin A at the NK-2 receptor. |
| Exact Mass |
551.211
|
|---|---|
| CAS # |
142001-63-6
|
| PubChem CID |
104974
|
| Appearance |
White to off-white solid powder
|
| Density |
1.26g/cm3
|
| Boiling Point |
734.7ºC at 760mmHg
|
| Flash Point |
398.1ºC
|
| Vapour Pressure |
1.91E-21mmHg at 25°C
|
| Index of Refraction |
1.628
|
| LogP |
6.695
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
38
|
| Complexity |
760
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(NC1(C2=CC=CC=C2)CCN(CC[C@@H](C3=CC(Cl)=C(Cl)C=C3)CN(C)C(C4=CC=CC=C4)=O)CC1)=O
|
| InChi Key |
PGKXDIMONUAMFR-AREMUKBSSA-N
|
| InChi Code |
InChI=1S/C31H35Cl2N3O2/c1-23(37)34-31(27-11-7-4-8-12-27)16-19-36(20-17-31)18-15-26(25-13-14-28(32)29(33)21-25)22-35(2)30(38)24-9-5-3-6-10-24/h3-14,21,26H,15-20,22H2,1-2H3,(H,34,37)/t26-/m1/s1
|
| Chemical Name |
(S)-N-(4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl)-N-methylbenzamide
|
| Synonyms |
SR-48968 SR489686 SR 489686
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~452.46 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.76 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 (3.76 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00429260 | COMPLETED | Drug: Saredutant | Depressive Disorder | Sanofi | 2007-01 | Phase 3 |
| NCT00250614 | COMPLETED | Drug: Saredutant succinate (SR48968C) | Depressive Disorder | Sanofi | 2005-04 | Phase 3 |
| NCT00250601 | COMPLETED | Drug: Saredutant succinate (SR48968C) | Depressive Disorder | Sanofi | 2005-04 | Phase 3 |
| NCT00390650 | COMPLETED | Drug: Saredutant | Anxiety | Sanofi | 2006-10 | Phase 3 |
| NCT00256113 | COMPLETED | Drug: Saredutant succinate (SR48968C) | Depressive Disorder | Sanofi | 2004-12 | Phase 3 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
