1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Carcinine dihydrochloride

Carcinine dihydrochloride  (Synonyms: β-Alanylhistamine dihydrochloride)

Cat. No.: HY-107567B Purity: 99.39%
Handling Instructions Technical Support

Carcinine (β-Alanylhistamine) dihydrochloride is the dihydrochloride salt of Carcinine (HY-107567). Carcinine is a selective and orally active histamine H3 receptor antagonist with a Ki of 0.2939 μM. Carcinine can reduce histamine content. Carcinine exhibits anti-oxidant activity and neuroprotective effects. Carcinine shows positive inotropic effect and can reduce blood sugar and blood lipid levels. Carcinine can be used for the researches of inflammation, neurological, cardiovascular and metabolic disease, such as retinal damage, seizure and diabetes.

For research use only. We do not sell to patients.

Carcinine dihydrochloride

Carcinine dihydrochloride Chemical Structure

CAS No. : 57022-38-5

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Based on 1 publication(s) in Google Scholar

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Description

Carcinine (β-Alanylhistamine) dihydrochloride is the dihydrochloride salt of Carcinine (HY-107567). Carcinine is a selective and orally active histamine H3 receptor antagonist with a Ki of 0.2939 μM. Carcinine can reduce histamine content. Carcinine exhibits anti-oxidant activity and neuroprotective effects. Carcinine shows positive inotropic effect and can reduce blood sugar and blood lipid levels. Carcinine can be used for the researches of inflammation, neurological, cardiovascular and metabolic disease, such as retinal damage, seizure and diabetes[1][2][3][4][5].

IC50 & Target[1]

H3 receptor

0.2939 μM (Ki)

H2 Receptor

365.3 μM (Ki)

H1 Receptor

3621.2 μM (Ki)

In Vitro

Carcinine (0.5 mM, 16 h) dihydrochloride forms a stable adduct with 4-HNE (HY-113466) a retention time of 17.5 mins[1].
Carcinine (1 μg-2 mg, 90 mins) dihydrochloride inhibits 4-HNE-induced modification of mouse retinal proteins with an IC50 of 33.2 μg/μL[1].
Carcinine (1 mg, 0-72 h) dihydrochloride reverses pre-formed 4-HNE-retinal protein adducts[1].
Carcinine (5 mM, 4-8 h) dihydrochloride rescues the protein level of retinol dehydrogenase 12 in mouse retinal explants treated with 4-HNE[1].
Carcinine dihydrochloride shows high affinity for histamine H3 receptor (Ki = 0.2939 μM) and extremely low affinity for H1 (Ki = 3621.2 μM) and H2 (Ki = 365.3 μM) receptors[2].
Carcinine (2-50 μM, 22.5 mins) dihydrochloride increases K+-induced endogenous 5-HT release but shows no effect on dopamine release in mouse forebrain slices[2].
Carcinine (10 mM) dihydrochloride scavenges hydroxyl radicals and inhibits deoxyribose damage[3].
Carcinine (10-25 mM, 60 mins) dihydrochloride reduces linoleic acid 13-monohydroperoxide (LOOH) and phosphatidylcholine hydroperoxide (PCOOH) in PC liposomes to hydroxy products (LOH)[3].

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

In Vivo

Carcinine (2 M, 1 μL per eye, intravitreally injection, 48 h recovery before light exposure) dihydrochloride protects retinal photoreceptors in BALB/c mice with bright light exposure[1].
Carcinine (0.2-20 mg/mouse, i.g., daily for 5 days) dihydrochloride protects the retina in BALB/c mice with bright light exposure[1].
Carcinine (5-50 mg/kg, i.p.) dihydrochloride decreases cortical and midbrain histamine content in ICR mice[2].
Carcinine (2-20 mg/kg, i.p., before PTZ) dihydrochloride significantly reduces the seizure stage induced by pentylenetetrazole (PTZ) in ICR mice[2].
Carcinine (10-20 mg/kg, i.p., 30 mins before scopolamine) dihydrochloride significantly ameliorates Scopolamine (HY-N0296)-induced learning deficit in ICR mice[2].
Carcinine (10-50 mg/kg, i.p.) dihydrochloride increases the total ambulation distance in ICR mice[2].
Carcinine (10-100 μg, heart injection via perfusate cannula) dihydrochloride shows positive inotropic effect in guinea pigs[4].

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

Animal Model: BALB/c mice with bright light exposure[1]
Dosage: 0.2, 2 and 20 mg/mouse
Administration: Orally gavage, daily for 5 days
Result: Showed that the rod a-wave amplitude increases from 84 μV to 257 μV, and the b-wave increaseed from 183 μV to 606 μV.
Decreased the loss rate of photoreceptor nuclei.
Prevented light-induced reduction of RDH12 protein level.
Animal Model: Pentylenetetrazole (PTZ)-induced kindling mice models[2]
Dosage: 2, 10 and 20 mg/kg
Administration: Intraperitoneally injection, before PTZ
Result: Reduced the seizure stage.
Prolonged the latency to myoclonic jerks and latency to generalized clonic seizures.
Molecular Weight

255.14

Formula

C8H16Cl2N4O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCC1=CN=CN1)CCN.[H]Cl.[H]Cl

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
In Vitro: 

H2O : 175 mg/mL (685.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9194 mL 19.5971 mL 39.1942 mL
5 mM 0.7839 mL 3.9194 mL 7.8388 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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

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(per animal)

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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
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
H2O 1 mM 3.9194 mL 19.5971 mL 39.1942 mL 97.9854 mL
5 mM 0.7839 mL 3.9194 mL 7.8388 mL 19.5971 mL
10 mM 0.3919 mL 1.9597 mL 3.9194 mL 9.7985 mL
15 mM 0.2613 mL 1.3065 mL 2.6129 mL 6.5324 mL
20 mM 0.1960 mL 0.9799 mL 1.9597 mL 4.8993 mL
25 mM 0.1568 mL 0.7839 mL 1.5678 mL 3.9194 mL
30 mM 0.1306 mL 0.6532 mL 1.3065 mL 3.2662 mL
40 mM 0.0980 mL 0.4899 mL 0.9799 mL 2.4496 mL
50 mM 0.0784 mL 0.3919 mL 0.7839 mL 1.9597 mL
60 mM 0.0653 mL 0.3266 mL 0.6532 mL 1.6331 mL
80 mM 0.0490 mL 0.2450 mL 0.4899 mL 1.2248 mL
100 mM 0.0392 mL 0.1960 mL 0.3919 mL 0.9799 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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  • 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.

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Carcinine dihydrochloride
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