| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
The binding affinities of sarnanserin/sarnanserin hydrochloride are observed for HCoV-229E 3CLpro and SARS-CoV 3CLpro. The KD value for human coronavirus 229E is 18.2 μM/36.6 μM (HCoV-229E) 3CLpro, while for SARS-related coronavirus (SARS-CoV) 3CLpro, it is 49.4 μM/78.0 μM[1]. Inhibiting the catalytic activity of SARS-CoV 3CLpro, the computed IC50 values of sarnanserin and sarnanserin hydrochloride are 4.92 μM and 5.05 μM, respectively. The comparable IC50 values of HCoV-229E 3CLpro are 4.68 μM and 5.68 μM. At doses up to 200 μM, none of these substances exhibit inhibitory effect against HRV-14 3Cpro [1].
|
|---|---|
| ln Vivo |
Cinnamonin (5 mg/kg; intravenous injection; 2 hours duration; male Wistar rats) treatment dramatically reduced systemic burn edema to shamburn levels. Administration of cinnamon significantly decreases leukocyte-endothelial interactions [2].
|
| Animal Protocol |
Animal/Disease Models: Male Wistar rat (250 g) thermal injury [2]
Doses: 5 mg/kg Route of Administration: intravenous (iv) (iv)injection; lasted 2 hrs (hrs (hours)). Experimental Results: Whole body burn edema was Dramatically diminished to shamburn levels. |
| References |
|
| Additional Infomation |
Cinanserin hydrochloride is the hydrochloride salt of cinanserin. It is an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus (SARS-Cov) and reduces virus replication in vitro. It has a role as an antiviral agent, an EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor and an anticoronaviral agent. It contains a cinanserin(1+).
A serotonin antagonist with limited antihistaminic, anticholinergic, and immunosuppressive activity. |
| Molecular Formula |
C20H25CLN2OS
|
|---|---|
| Molecular Weight |
376.94
|
| Exact Mass |
376.138
|
| CAS # |
54-84-2
|
| Related CAS # |
1166-34-3 (Parent)
|
| PubChem CID |
6433141
|
| Appearance |
Light yellow to yellow solid powder
|
| Boiling Point |
519.5ºC at 760mmHg
|
| Flash Point |
268ºC
|
| LogP |
5.257
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
25
|
| Complexity |
391
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CCCSC1=CC=CC=C1NC(=O)/C=C/C2=CC=CC=C2.Cl
|
| InChi Key |
LXGJPDKYMJJWRB-IERUDJENSA-N
|
| InChi Code |
InChI=1S/C20H24N2OS.ClH/c1-22(2)15-8-16-24-19-12-7-6-11-18(19)21-20(23)14-13-17-9-4-3-5-10-17;/h3-7,9-14H,8,15-16H2,1-2H3,(H,21,23);1H/b14-13+;
|
| Chemical Name |
(E)-N-[2-[3-(dimethylamino)propylsulfanyl]phenyl]-3-phenylprop-2-enamide;hydrochloride
|
| Synonyms |
Cinanserin HCl SQ-10643 Cinanserin Hydrochloride
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~125 mg/mL (~331.62 mM)
H2O : ~100 mg/mL (~265.29 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.52 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 (5.52 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 (5.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6529 mL | 13.2647 mL | 26.5294 mL | |
| 5 mM | 0.5306 mL | 2.6529 mL | 5.3059 mL | |
| 10 mM | 0.2653 mL | 1.3265 mL | 2.6529 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
