2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. CGP 36742

CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a blood-brain barrier (BBB) penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study.

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CGP 36742 Chemical Structure

CGP 36742 Chemical Structure

CAS No. : 123690-78-8

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Based on 1 publication(s) in Google Scholar

CGP 36742 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CGP 36742

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Description

CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a blood-brain barrier (BBB) penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study[1][2][3][4].

IC50 & Target

IC50: 32 μM (GABAB)[1]
Cellular Effect
Cell Line Type Value Description References
Oocyte IC50
38 μM
Compound: 7, CGP-36742
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
508 μM
Compound: 7, CGP-36742
Antagonist activity at human recombinant GABAA alpha1beta2gamma2L receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAA alpha1beta2gamma2L receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
62 μM
Compound: 7, CGP-36742
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
62 μM
Compound: 2, SGS742
Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
[PMID: 18528996]
In Vitro

CGP 36742 blocks the late inhibitory postsynaptic potential (i.p.s.p.) in CA1 pyramidal neurons[2].
CGP 36742 (1 μM) prevents kynurenate from antagonizing N-methyl-d-aspartate (NMDA) (HY-17551)-induced release of noradrenaline from rat brain slices potently[4].
CGP 36742 (1 μM) increases the somatostatin-like immunoreactivity (SRIF-LI) release from hippocampal slices exposed to NMDA[4].

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

CGP 36742 Related Antibodies
In Vivo

CGP 36742 (10-30 mg/kg; i.p.; 30 min before test) exhibits antidepressant-like activity in the forced swim test in mice[1].
CGP 36742 (10 mg/kg; i.p.; once daily for 14 d) are effective in an olfactory bulbectomy (OB) model of depression in rats[1].
CGP 36742 (30-200 mg/kg; p.o.; administered in a cumulative manner at intervals of 2.5-3 h) blocks the neuronal depression induced by iontophoretically applied baclofen in anaesthetized rats[2].
CGP 36742 (1-10 mg/kg; i.v.; 25-30 min before test) dose dependently attenuates paired-pulse inhibition measured at latencies of > 100 ms[2].
CGP 36742 (50-1000 mg/kg; i.v. or p.o.; once or twice) can penetrate the blood-brain barrier in male Sprague-Dawley rats [3].

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

Animal Model: Male Albino Swiss mice (22-26 g)[1]
Dosage: 10, 30 mg/kg
Administration: Intraperitoneal injection (i.p.); 30 min before test
Result: Significantly reduced the immobility time in the forced swim test at both doses (10 mg/kg by 32% and 30 mg/kg by 40%).
Had no effect on the spontaneous locomotor activity in mice.
Animal Model: Male Wistar rats (200-250 g), olfactory bulbectomy model[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.); once daily for 14 d
Result: Single administration did not alter the olfactory bulbectomy (OB)-induced learning deficit, induced following bulbectomy.
Restored the learning deficit in OB rats (five trials) without affecting performance in sham-operated animals.
Reduced the OB-related increase in the number of rearings + peepings.
Animal Model: Male rats (weighing 280-320 g)[2]
Dosage: 30-200 mg/kg
Administration: Oral gavage (p.o.); administered in a cumulative manner at intervals of 2.5-3 h.
Result: Antagonized baclofen-induced inhibitory effects on spontaneously firing cortical neurons in a dose-dependent manner.
Animal Model: Male Sprague-Dawley rats (200-325 g)[3]
Dosage: 50, 100, 200, 500, 1000 mg/kg
Administration: Intravenous injection (i.v.) via tail vein of 50, 100, 200 mg/kg, oral gavage (p.o.) of 500, 1000 mg.kg; in two rats given an i.v. injection of 100 mg/kg, a second i.v. injection of 100 mg/kg was given after 6 h and samples were collected for another 6 h.
Result: The appearance in the rat brain frontal cortex after i.v. injection was seen in the first 30 min dialyzate collected and peaked in the 1 h dialysate.
Removed or metabolized from brain in dialyzates collected 3 h post-injection.
The presence was again seen 30 min after the second 100 mg/kg i.v. injection administered 6 h after the first injection.
Showed the appearance in the third ventricle of the rat brain after two i.v. injections of 100 mg/kg with an interval of 6 h.
Showed that the highest concentrations were seen 1.5 or 2 h after the p.o..
Molecular Weight

179.20

Formula

C7H18NO2P
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=P(CCCN)(O)CCCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 125 mg/mL (697.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5804 mL 27.9018 mL 55.8036 mL
5 mM 1.1161 mL 5.5804 mL 11.1607 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. 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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  • 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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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: ≥98.0%

SDS (393 KB)

COA (241 KB) HNMR (191 KB) MS (72 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. 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 5.5804 mL 27.9018 mL 55.8036 mL 139.5089 mL
5 mM 1.1161 mL 5.5804 mL 11.1607 mL 27.9018 mL
10 mM 0.5580 mL 2.7902 mL 5.5804 mL 13.9509 mL
15 mM 0.3720 mL 1.8601 mL 3.7202 mL 9.3006 mL
20 mM 0.2790 mL 1.3951 mL 2.7902 mL 6.9754 mL
25 mM 0.2232 mL 1.1161 mL 2.2321 mL 5.5804 mL
30 mM 0.1860 mL 0.9301 mL 1.8601 mL 4.6503 mL
40 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4877 mL
50 mM 0.1116 mL 0.5580 mL 1.1161 mL 2.7902 mL
60 mM 0.0930 mL 0.4650 mL 0.9301 mL 2.3251 mL
80 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7439 mL
100 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3951 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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CGP 36742 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:

CGP 36742123690-78-8SGS-742CGP36742CGP-36742SGS742SGS 742GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorblood-barrierdepressionInhibitorinhibitorinhibit

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