LGD-2226

Name: LGD-2226
Brand: MedChemExpress
SKU: HY-105318
Rating: 4.5 (0 reviews)

Cat. No.: HY-105318 Purity: 98.58%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

LGD-2226 is a selective and orally active androgen receptor modulator with an EC₅₀ of 0.2 nM and a K_i of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

LGD-2226 화학구조

CAS No. : 328947-93-9

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	견적 받기
100 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of LGD-2226:

LGD-2226 (Standard) 견적 받기

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

EC50: 0.2 nM (Androgen receptor)^[1]; Ki: 1.5 nM (Androgen receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CV-1	EC₅₀	0.2 1 Compound: 13i	Agonist activity at human androgen receptor expressed in CV1 cells Agonist activity at human androgen receptor expressed in CV1 cells	[PMID: 17257838]
CV-1	EC₅₀	0.2 1 Compound: 13i	Agonist activity at human androgen receptor expressed in CV1 cells Agonist activity at human androgen receptor expressed in CV1 cells	[PMID: 17257838]
CV-1	EC₅₀	0.2 1 Compound: 4m, LGD2226	Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay	[PMID: 17034117]
CV-1	EC₅₀	0.2 1 Compound: 4m, LGD2226	Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay	[PMID: 17034117]
CV-1	IC₅₀	>10 3 Compound: 4m, LGD2226	Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay	[PMID: 17034117]
CV-1	IC₅₀	> 10000 1 Compound: 4m, LGD2226	Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay	[PMID: 17034117]

In Vitro

LGD-2226 (Compound 4m) occupies the same binding pocket as dihydrotestosterone (DHT), and in general, the protein backbone is superposable to that observed with DHT. Just like the carbonyl group of DHT, the quinolone carbonyl forms hydrogen bond interactions with GLN711 and ARG752. GLN711 forms an additional hydrogen bond with the quinolone NH of LGD-2226. The trifluoroethyl groups of LGD-2226 occupy the same space in the receptor as the C and D rings of the steroid^[1].

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

In Vivo

LGD-2226 (Compound 4m; 1-100 mg/kg; oral administration; daily; for 2 weeks; adult oORDX rats) has a pronounced effect on the levator ani muscle, maintaining the muscle weight at the eugonadal levels at an approximate 3 mg/kg dose. LGD-2226 has weak trophic effects on the prostate. An amount of 100 mg/kg LGD-2226 is required to maintain prostate weight at intact levels. These data clearly show the tissue selectivity of LGD-2226^[1].

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

Animal Model:	Adult orchidectomized (ORDX) rats^[1]
Dosage:	1-100 mg/kg
Administration:	Oral administration; daily; for 2 weeks
Result:	Had a pronounced effect on the levator ani muscle, maintaining the muscle weight at the eugonadal levels at an approximate 3 mg/kg dose.

분자량

392.22

화학식

C₁₄H₉F₉N₂O

CAS No.

328947-93-9

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1NC2=C(C=C(N(CC(F)(F)F)CC(F)(F)F)C=C2)C(C(F)(F)F)=C1

선적

Room temperature in continental US; may vary elsewhere.

보관

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

용액&용해도

In Vitro:

DMSO : 125 mg/mL (318.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5496 mL	12.7479 mL	25.4959 mL
5 mM	0.5099 mL	2.5496 mL	5.0992 mL
10 mM	0.2550 mL	1.2748 mL	2.5496 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

순도&문서

Purity: 98.58%

Select Batch:

Data Sheet (276 KB) SDS (419 KB)

COA (253 KB) HNMR (259 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. van Oeveren A, et al. Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator. J Med Chem. 2006 Oct 19;49(21):6143-6. [Content Brief]

[2]. Miner JN, et al. An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate. Endocrinology. 2007 Jan;148(1):363-73. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5496 mL	12.7479 mL	25.4959 mL	63.7397 mL
	5 mM	0.5099 mL	2.5496 mL	5.0992 mL	12.7479 mL
	10 mM	0.2550 mL	1.2748 mL	2.5496 mL	6.3740 mL
	15 mM	0.1700 mL	0.8499 mL	1.6997 mL	4.2493 mL
	20 mM	0.1275 mL	0.6374 mL	1.2748 mL	3.1870 mL
	25 mM	0.1020 mL	0.5099 mL	1.0198 mL	2.5496 mL
	30 mM	0.0850 mL	0.4249 mL	0.8499 mL	2.1247 mL
	40 mM	0.0637 mL	0.3187 mL	0.6374 mL	1.5935 mL
	50 mM	0.0510 mL	0.2550 mL	0.5099 mL	1.2748 mL
	60 mM	0.0425 mL	0.2125 mL	0.4249 mL	1.0623 mL
	80 mM	0.0319 mL	0.1593 mL	0.3187 mL	0.7967 mL
	100 mM	0.0255 mL	0.1275 mL	0.2550 mL	0.6374 mL

LGD-2226 Related Classifications

Metabolic Disease Endocrinology

Help & FAQs

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:

LGD-2226328947-93-9LGD2226LGD 2226Androgen ReceptorDihydrotestosteroneorally levatoranimuscletissueselectivitynonsteroidalGLN711wastingosteoporosisInhibitorinhibitorinhibit

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LGD-2226

고객리뷰

Other Forms of LGD-2226:

LGD-2226 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

순도&문서

References

고객리뷰

LGD-2226 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

LGD-2226 Related Classifications

Keywords:

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고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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