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Cat. No.: HY-180372

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CSP-2503

CSP-2503 is a potent and selective 5-HT_1A receptor agonist , with an EC₅₀ of 0.15 μM and a K_i of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (K_i > 1000 nM), 5-HT₄ receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 581813-10-7
화학식: C₂₂H₂₆N₄O₂
분자량:378.48

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

CSP-2503 Chemical Structure

CAS No.: 581813-10-7

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocol (1)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

5-HT_1A Receptor

0.15 μM (EC₅₀)

5-HT_1A Receptor

4.1 nM (Ki)

5-HT_2A Receptor

13.5 nM (Ki)

5-HT₃ Receptor

8.9 nM (Ki)

5-HT₄ Receptor

>10000 nM (Ki)

5-HT₇ Receptor

100.9 nM (Ki)

α1-adrenergic receptor

>1000 nM (Ki)

serotonin transporter

976.3 nM (Ki)

benzodiazepine receptor

>10000 nM (Ki)

Dopamine D2 receptor

192.1 nM (Ki)

All 5-HT Receptor Isoforms :

All Adrenergic Receptor Isoforms :

All Dopamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	0.15 μM Compound: 9 (S)	Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells	[PMID: 15801844]

In Vitro

CSP-2503 inhibits Forskolin (HY-15371)-induced cAMP increase in a dose-dependent manner with an EC₅₀ of 0.15 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

CSP-2503 (10 mg/kg; s.c.; single dose) exhibits anxiolytic activity in mice^[1].
CSP-2503 (2.5-20 mg/kg; s.c.; single dose) acts as a somatodendritic 5-HT_1A receptor agonist in mice^[1].

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

Animal Model:

Mice^[1]
Dosage:

10 mg/kg
Administration:

s.c.; single dose
Result:

Increased time spent in the lit area to 155.4 seconds compared to 83 seconds in vehicle-treated mice.
Increased time spent in the lit area by 87.2%.

Animal Model:

Mice hypothermia model^[1]
Dosage:

2.5, 5, 10, 20 mg/kg
Administration:

s.c.; single dose
Result:

Induced a dose-related decrease in rectal temperature.
Decreased the 5-HIAA/5-HT ratio in mouse hypothalamus.

Chemical Information

CAS No. 581813-10-7
분자량 378.48
화학식 C₂₂H₂₆N₄O₂
SMILES

C(N1CCN(C=2C3=C(C=CC2)C=CC=C3)CC1)N4C(=O)[C@]5(N(C(=O)C4)CCC5)[H]
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocol

All Animals and Diseases

Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. López-Rodríguez ML, et al. Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist. Bioorg Med Chem Lett. 2003;13(8):1429-1432. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocol
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

CSP-2503

All 5-HT Receptor Isoforms

All Adrenergic Receptor Isoforms

All Dopamine Receptor Isoforms