2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. α-Casozepine

α-Casozepine is an orally effective anxiolytic that binds to the benzodiazepine site of the GABAA receptor in bovine samples with an IC50 of 88 μM. α-Casozepine exerts anxiolytic and anti-stress effects on cats exposed to unfamiliar environments and dogs undergoing road transport. α-Casozepine exhibits significant anxiolytic activity in rats. α-Casozepine can be used in studies related to fear, anxiety and stress.

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α-Casozepine

α-Casozepine Chemical Structure

CAS No. : 117592-45-7

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Based on 1 publication(s) in Google Scholar

α-Casozepine Related Antibodies

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Description

α-Casozepine is an orally effective anxiolytic that binds to the benzodiazepine site of the GABAA receptor in bovine samples with an IC50 of 88 μM. α-Casozepine exerts anxiolytic and anti-stress effects on cats exposed to unfamiliar environments and dogs undergoing road transport. α-Casozepine exhibits significant anxiolytic activity in rats. α-Casozepine can be used in studies related to fear, anxiety and stress[1][2][3].

In Vivo

α-Casozepine (included in the complete Royal Canin Adult Calm Formula; administered orally; twice daily; for 4 weeks) exerts an anxiolytic effect on cats exposed to a novel environment, but does not reduce the fear response of cats to unfamiliar humans[1].
Combined with cannabidiol (CBD) and L-Tryptophan (HY-N0623), α-Casozepine (21.2-32.1 mg/kg BW; p.o.; single administration) exerts mild anti-stress effects in dogs subjected to road transportation, as evidenced by a significantly smaller increase in post-stress serum cortisol levels compared with the placebo group[2].
α-Casozepine (0.4 mg/kg; i.p.; single administration) exhibits significant anxiolytic activity in the conditioned defensive burying paradigm of Wistar rats[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Domestic shorthair cats (5 neutered males, 7 spayed females, 7 intact females; age 4-12 years)[1]
Dosage: Included in complete Royal Canin Feline Calm diet
Administration: oral; twice daily; 4 weeks
Result: Showed non-significant increase in distance traveled from baseline to test 1 and test 2, whereas control cats showed significant or marginally significant decreases.
Showed marginally not significant decrease in inactivity duration from baseline to test 1, and non-significant decrease from baseline to test 2.
Showed statistically significant increase in inactivity frequency from baseline to test 1, and non-significant increase from baseline to test 2.
Exhibited no significant changes in home room test or human interaction test compared to baseline.
Animal Model: Norfolk Terrier, Beagle, Labrador Retriever (healthy adult, 3.6 years mean age, 3.6-36.0 kg weight range, 55.6% neutered male, 44.4% female [21 spayed, 3 entire])[2]
Dosage: 21.2-32.1 mg/kg BW (mean 24.2 mg/kg BW; co-administered with mean 1.8 mg/kg BW CBD and 14.3 mg/kg BW L-tryptophan)
Administration: oral; single dose
Result: Reduced serum cortisol increase from baseline to post-stress paradigm by a mean difference of -7.01 ng/mL compared to placebo.
Showed a non-significant trend for reduced lip licking compared to placebo.
Showed a non-significant trend for lower activity points compared to placebo.
Exerted no significant effects on heart rate, heart rate variability, body position, movement, whining, panting, or qualitative arousal ratings compared to placebo.
Animal Model: Wistar rats[3]
Dosage: 0.4 mg/kg
Administration: i.p.; single dose
Result: Decreased the duration of probe burying compared to saline.
Reduced the ratio of retreats to approaches toward the probe.
Exerted effects comparable to those induced by 1 mg/kg diazepam.
Molecular Weight

1267.47

Formula

C60H94N14O16
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-Leu-Gly-Tyr-Leu-Glu-Gln-Leu-Leu-Arg
Sequence Shortening

YLGYLEQLLR
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 66.67 mg/mL (52.60 mM; ultrasonic and adjust pH to 2 with 1 M HCl)

DMSO : 20 mg/mL (15.78 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7890 mL 3.9449 mL 7.8897 mL
5 mM 0.1578 mL 0.7890 mL 1.5779 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.36%

SDS (252 KB)

COA (247 KB) RP-HPLC (390 KB) MS (123 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 0.7890 mL 3.9449 mL 7.8897 mL 19.7243 mL
5 mM 0.1578 mL 0.7890 mL 1.5779 mL 3.9449 mL
10 mM 0.0789 mL 0.3945 mL 0.7890 mL 1.9724 mL
15 mM 0.0526 mL 0.2630 mL 0.5260 mL 1.3150 mL
H2O 20 mM 0.0394 mL 0.1972 mL 0.3945 mL 0.9862 mL
25 mM 0.0316 mL 0.1578 mL 0.3156 mL 0.7890 mL
30 mM 0.0263 mL 0.1315 mL 0.2630 mL 0.6575 mL
40 mM 0.0197 mL 0.0986 mL 0.1972 mL 0.4931 mL
50 mM 0.0158 mL 0.0789 mL 0.1578 mL 0.3945 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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α-Casozepine Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

α-Casozepine117592-45-7GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptoranxiolyticdogsGABAA receptorbovine cerebral cortex membranesMA-10 mouse Leydig cellsWistar ratscortisolcatsfearanxiety and stressInhibitorinhibitorinhibit

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