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製品番号: HY-178760

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TGF-8027

TGF-8027 is a selective 5-HT_2A receptor agonist with a K_i of 7.4 nM and an EC₅₀ of 3.3 nM at the human receptor. TGF-8027 activates the 5-HT_2A receptor-mediated Gq protein signaling pathway. TGF-8027 induces dose-dependent head-twitch responses in mice.

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CAS 番号: 3136748-24-5
分子式: C₁₉H₂₂N₂O₃
分子量:326.39

保管条件:

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

Data Sheet (282 KB)

TGF-8027 構造式

CAS 番号: 3136748-24-5

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

IC₅₀ & Target

^[1]

5-HT_2A Receptor

7.4 nM (Ki)

5-HT_2A Receptor

3.3 nM (EC₅₀)

5-HT Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

TGF-8027 (compound 1) (60 minutes at 37°C) is a 5-HT_2A agonist in HEK293T cells with an EC₅₀ of 3.3 nM and 48.5-fold selectivity over 5-HT_2C in the Gq dissociation BRET assay^[1].
TGF-8027 (60 minutes at 37°C) shows 368-fold selectivity for 5-HT_2A over 5-HT_2C VGV in the Gq dissociation BRET assay in HEK293T cells^[1].
TGF-8027 (60 minutes at 37°C) has an EC₅₀ of 14 nM for mouse 5-HT_2A in HEK293T cells and shows reduced selectivity for mouse 5-HT_2C^[1].
TGF-8027 exhibits 85-fold selectivity for 5-HT_2A over 5-HT_2C in calcium flux assays in Flp-In 293 T-Rex cells^[1].
TGF-8027 (60 minutes at 37°C) recruits β-arrestin2 at 5-HT_2A in HEK293T cells with an EC₅₀ of 4.5 nM and an E_max of 108%^[1].
TGF-8027 binds to human 5-HT_2A with an affinity of 7.4 nM and exhibits 149-fold selectivity for 5-HT_2A over 5-HT_2C in a cell-free radioligand binding assay^[1].

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

体内実験

TGF-8027 (Compound 1) (5 mL/kg; subcutaneous injection; single injection per test; 30-minute recording period) dose-dependently induces 5-HT_2A-mediated head-twitch behavior in mice, with an ED₅₀ of 1.86 mg/kg^[1].

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

Animal Model:

C57BL/6J (male, 6-8 weeks old)^[1]
Dosage:

5 mL/kg
Administration:

s.c.; single injection per test session; 30-minute recording period
Result:

The ED₅₀ was 1.86 mg/kg (95% CI 1.18-2.92).

化学情報

CAS 番号 3136748-24-5
分子量 326.39
分子式 C₁₉H₂₂N₂O₃
SMILES

COC1=C(CCNC(C)C2=CC=CC=C2O)C=C(OC)C(C#N)=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Fenske TG, et al. Discovery of Highly Selective 5-HT Agonists Using Structure-Guided Design. Journal of medicinal chemistry. 2025 Oct 09;68(19):20619-20635. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

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MOQ

Minimum order quantity

100 mg

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