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製品番号: HY-116453

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RO5527239

RO5527239 is an orally active TGR5 agonist, that induces a stimulatory response from intestinal L cells and specificially secrets the endogenous hormone GLP-2.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1354812-99-9
分子式: C₂₈H₃₁N₃O₃
分子量:457.56

保管条件:

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

Data Sheet (270 KB)

RO5527239 構造式

CAS 番号: 1354812-99-9

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

RO5527239 is an orally active TGR5 agonist, that induces a stimulatory response from intestinal L cells and specificially secrets the endogenous hormone GLP-2^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.004 μM Compound: (R)-29, RO5527239	Agonist activity at recombinant human GPBAR1 expressed in CHO cells Agonist activity at recombinant human GPBAR1 expressed in CHO cells	[PMID: 23831134]
CHO	EC₅₀	0.028 μM Compound: (R)-29, RO5527239	Agonist activity at recombinant mouse GPBAR1 expressed in CHO cells Agonist activity at recombinant mouse GPBAR1 expressed in CHO cells	[PMID: 23831134]
NCI-H716	EC₅₀	0.08 μM Compound: (R)-29, RO5527239	Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production	[PMID: 23831134]

体内実験

RO5527239 (30 mg/kg, p.o. for 10 days) stimulates the TGR5 receptor, upregulates L cells and L cells hormone GLP-2, triggers a GLP-2-dependent intestinal adaption in C57BL/6N mice^[1].

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

Animal Model:

GLP-2r^-/- and GLP-2r^+/+ C57Bl/6N mice^[1]
Dosage:

30 mg/kg
Administration:

p.o. for 10 days
Result:

Increased GLP-1 and GLP-2 concentrations in the colon, gallbladder weight with both genotype. Increased villus height in the duodenum and decreased colon length in GLP-2r^+/+ mice.

化学情報

CAS 番号 1354812-99-9
分子量 457.56
分子式 C₂₈H₃₁N₃O₃
SMILES

O=C(C1CCN(C2=CC=C([C@H](C3=CC=CC=C3C)C/C(C4=CC(C)=NC=C4)=N\O)C=C2)CC1)O
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.

プロトコル

All Signal Pathway Related

Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.

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 (270 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]. Hunt JE, et al., Pharmacological activation of TGR5 promotes intestinal growth via a GLP-2-dependent pathway in mice. Am J Physiol Gastrointest Liver Physiol. 2020 May 1;318(5):G980-G987. [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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