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Metformin Hydrochloride Antihyperglycemic agent

Name: Metformin Hydrochloride
Brand: Selleck Chemicals
SKU: S1950
Rating: 5 (105 reviews)

제품 번호: S1950

Metformin Hydrochloride (1,1-Dimethylbiguanide Hydrochloride) is a highly effective Antihyperglycemic Agent, which primarily decreases hyperglycemia in hepatocytes by suppressing hepatic gluconeogenesis (glucose production by the liver). It also promotes mitophagy in mononuclear cells and induces apoptosis of lung cancer cells through activating the JNK/p38 MAPK pathway and GADD153.

Metformin Hydrochloride Carbohydrate Metabolism chemical Chemical Structure

화학 구조

분자량: 165.62

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품질 관리 (Quality Control)

배치: 순도: 99.99%

99.99

함께 자주 사용되는 제품 Metformin Hydrochloride

Melatonin

It and Melatonin are effective in reduction of plasmatic levels of liver enzymes and decrease inflammatory response in rats.

관련 타겟	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Mitochondrial Metabolism Casein Kinase
기타 Carbohydrate Metabolism 억제제	2-DG (2-Deoxy-D-glucose) Bromopyruvic acid (3-BP) Dorzagliatin LY2608204 Voglibose 1-Deoxynojirimycin 4',7-Dimethoxy-5-Hydroxyflavone AZD1656 Nodakenetin Kaempferol-3-O-neohesperidoside

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
human HepG2 cells	Function assay	1 mM	24 h	Activation of AMPK in human HepG2 cells assessed as reduction of gluconeogenesis at 1 mM after 24 hrs by enzymatic colorimetric assay	26471090
mouse 3T3L1 cells	Function assay	1 mM		Induction of AMPK phosphorylation in mouse 3T3L1 cells at 1 mM by Western blot analysis	25216379
human HepG2 cells	Function assay	1 mM	24 h	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 1 mM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose	23025244
human MDA-MB-231 cells	Function assay	1 to 20 mM	24 h	Antiproliferative activity against human MDA-MB-231 cells at 1 to 20 mM after 24 hrs by MTT assay.	22459208
human HepG2 cells	Function assay		24 h	Increase in glucose consumption in insulin-resistant human HepG2 cells after 24 hrs, EC50=0.27 μM.	21856048
Hs575T	Function assay	20 mM	24 hrs	Inhibition of mTOR phosphorylation in triple-negative human Hs575T cells at 20 mM after 24 hrs by immunoblot analysis	23490148
Hs578T	Antiinvasive assay	20 mM	17 hrs	Antiinvasive activity against triple-negative human Hs578T cells at 20 mM after 17 hrs by light microscopic analysis	23490148
Hs575T	Function assay	20 mM	24 hrs	Activation of AMPK in triple-negative human Hs575T cells at 20 mM after 24 hrs by immunoblot analysis	23490148
L6	Function assay	2 mM	4 hrs	Increase in glucose uptake in rat L6 cells at 2 mM treated for 4 hrs post 30 mins AMPK inhibitor compound C treatment	29128163
HepG2	Function assay	1 mM	24 hrs	Induction of glucose consumption in human HepG2 cells at 1 mM incubated for 24 hrs	28651984
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	165.62	화학식	C₄H₁₁N₅.HCl	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1115-70-4	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	1,1-Dimethylbiguanide HCl			Smiles	CN(C)C(=N)N=C(N)N.Cl

용해도 (Solubility)

In vitro
배치:

Water : 33 mg/mL

Ethanol : Insoluble

Water : 200 mg/mL

DMSO : 100 mg/mL (603.79 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : Insoluble

Water : 33 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.300mg/ml (13.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 46 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC₅₀/Ki	AMPK (Hepatocytes)
시험관 내(In vitro)	Metformin (500 μM) activates AMPK in hepatocytes, as a result, acetyl-CoA carboxylase (ACC) activity is reduced, fatty acid oxidation is induced, and expression of lipogenic enzymes is suppressed. Metformin (2 mM) activates muscle AMPK and promotes glucose uptake. Metformin (500 μM) or AICAR strongly suppresses SREBP-1 mRNA expression in rat hepatocytes. Metformin ameliorates hyperglycemia without stimulating insulin secretion, promoting weight gain, or causing hypoglycemia. Metformin has beneficial effects on circulating lipids linked to increased cardiovascular risk. Metformin decreases hepatic glucose production and increases skeletal myocyte glucose uptake. Metformin requires LKB1 in the liver to lower blood glucose levels. Metformin (2 mM) leads to a significant increase in the activity of both α1- and α2-containing complexes in muscle cells. Metformin (2 mM) also increases threonine 172 phosphorylation in muscle cells.
생체 내(In vivo)	Metformin (100 mg/ml, po) treatment produces significant decreases in hepatic expression of mRNAs for SREBP-1, FAS, and S14 in SD rats that are consistent with effects documented in cells. Metformin also decreases hepatic lipids in obese mice. Metformin (250 mg/kg, i.p.) increases AMPK phosphorylation in livers of wild-type mice. Metformin (250 mg/kg, i.p.) treatment reduces blood glucose by more than 50% in the wild-type mice on a high-fat diet. Metformin (250 mg/kg, i.p.) treatment also loweres blood glucose in the ob/ob mice by 40%.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/11602624/ [2] https://pubmed.ncbi.nlm.nih.gov/16308421/ [3] https://pubmed.ncbi.nlm.nih.gov/11994296/ [4] https://pubmed.ncbi.nlm.nih.gov/17477363/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	pSTAT3 (Ser727) / STAT3 / Jak2 / Cdk5 / pNFκB / Bcl-2 / Bcl-XL / c-Myc pACC / ACC / pS6 / S6 TTP / p-STAT3 / STAT3 / c-Myc p-AMPK / AMPK / p-mTOR / mTOR / p-S6K / S6K	28114390
Immunofluorescence	beta-catenin / AMPK CD86 / CD206 PAR LKB1	30854043
Growth inhibition assay	Cell viability	26956973

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT05910554	Not yet recruiting	Sarcoidosis Pulmonary	University of Maryland Baltimore	May 1 2024	Phase 2
NCT06120881	Recruiting	Type 2 Diabetes	University of California San Francisco\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	April 1 2024	Early Phase 1
NCT06147050	Not yet recruiting	Long COVID	Purpose Life Sciences	April 2024	Phase 3
NCT06296836	Not yet recruiting	Diabetes Mellitus Type 2	University of Illinois at Chicago\|Emily Hanners\|Dulal Bhaumik\|Avisek Datta\|Peggy Choye\|Hailey Soni\|Annesti Elmasri\|Julie Jun\|Colin Goodman	April 1 2024	Phase 4

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Metformin Hydrochloride Antihyperglycemic agent

화학 구조

분자량: 165.62

품질 관리 (Quality Control)

함께 자주 사용되는 제품 Metformin Hydrochloride

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)