Chlorcyclizine (hydrochloride) (Synonyms: NSC 169496) |
| Catalog No.GC13465 |
histamine H1 receptor antagonist and inhibits HCV
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 14362-31-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Chlorcyclizine is a phenylpiperazine antagonist for histamine H1 receptor [1].
The histamine has been involved in modulating many physiological functions of the hypothalamus, such as arousal state, feeding, locomotor activity, and drinking. Histamine has been involved in circadian rhythm of locomotor activity and exploratory behavior through H1R [1].
In vitro: The Ki value of chlorcyclizine for histamine H1 receptor was 9 nM [1]. Chlorcyclizin was effective against hepatitis C virus (HCV) with an EC50 of 44 nM, preventing viral entry into host cells [2].
In vivo: In chimeric mice xenografted with primary human hepatocytes, chlorcyclizine (10-50 mg/kg) significantly inhibited infection of HCV genotypes 1b and 2a [2]. Chlorcyclizine induced a resistance to sodium pentobarbital anesthesia. Intraperitoneal injection of chlorcyclizine showed a sedative effect in small doses, but a convulsive effect in large doses. Intraperitoneal injections of the drug did not affect the recovery time from pentobarbital anesthesia [3]. In rats, pretreatment with chlorcyclizine for several days shortened the duration of action of a subsequent dose of hexobarbital, pentobarbital or zoxazolamine, and accelerated in vivo metabolism of hexobarbital [4]. The administration of chlorcyclizine (50 g/kg) to rats by stomach tube daily for 1 week resulted in significant increases in liver weight, microsomal protein concentration and the activity of the NADPH-dependent hepatic microsomal ethanol-oxidizing system (MEOS) [5].
References:
[1] Tran V T, Chang R S, Snyder S H. Histamine H1 receptors identified in mammalian brain membranes with [3H] mepyramine[J]. Proceedings of the National Academy of Sciences, 1978, 75(12): 6290-6294.
[2] He, S. ,Xiao, J.,Dulcey, A.E., et al. Discovery, optimization, and characterization of novel chlorcyclizine derivatives for the treatment of hepatitis C virus infection. Journal of Medicinal Chemistry 59(3), 841-853 (2016).
[3] Thompson I D, Dolowy W C, Cole W H. Development of a resistance to sodium pentobarbital in rats fed on a diet containing chlorcyclizine hydrochloride[J]. Journal of Pharmacology and Experimental Therapeutics, 1959, 127(2): 164-166.
[4] Conney A H, Burns J J, Michaelson I A. Stimulatory effect of chlorcyclizine on barbiturate metabolism[J]. Journal of Pharmacology and Experimental Therapeutics, 1961, 132(2): 202-206.
[5] Khanna J M, Kalant H, Lin G. Significance in vivo of the increase in micro-somal ethanol-oxidizing system after chronic administration of ethanol, pheno-barbital and chlorcyclizine[J]. Biochemical pharmacology, 1972, 21(16): 2215-2226.
Animal experiment: | Rats[1]Timed-mated CRL:CD [SD] female rats between 9 and 13 weeks of age at initiation of dosing and weighing between 245 and 363 g are used. Rats are administered a single daily oral gavage dose of 30, 60, or 90 mg/kg Chlorcyclizine (n=8/group) during the sensitive period for palate development, GDs 11 to 14. These doses are selected such that 30 mg/kg is a likely no-effect dose and higher doses of 60 and/or 90 mg/kg will induce a moderate or high incidence of fetal cleft palate. Given that CRL:CDs [SD] rats have an extremely low incidence of spontaneous cleft palate in the testing laboratory, as well as to avoid unnecessary use of animals, a methylcellulose control group is omitted[1]. |
References: [1]. Enright BP, et al. Effects of the histamine H1 antagonist Chlorcyclizine on rat fetal palate development. Birth Defects Res B Dev Reprod Toxicol. 2010 Dec;89(6):474-84. | |
| Cas No. | 14362-31-3 | SDF | |
| Synonymes | NSC 169496 | ||
| Chemical Name | 1-[(4-chlorophenyl)phenylmethyl]-4-methyl-piperazine, monohydrochloride | ||
| Canonical SMILES | CN1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1.Cl | ||
| Formula | C18H21ClN2 • HCl | M.Wt | 337.3 |
| Solubility | ≥ 11mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9647 mL | 14.8236 mL | 29.6472 mL |
| 5 mM | 592.9 μL | 2.9647 mL | 5.9294 mL |
| 10 mM | 296.5 μL | 1.4824 mL | 2.9647 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *