Name: Orlistat
Brand: Selleck Chemicals
SKU: S1629
Rating: 5 (18 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.98%

99.98

관련 타겟	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
기타 Lipase 억제제	Tanshinone IIA Atglistatin JZL184 Pristimerin Schaftoside ABX-1431 XEN445 Cetilistat Pancreatin URB602

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

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
HEK293T	Function assay			Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay, IC50=0.01 μM	22738638
COS	Function assay		15 mins	Inhibition of human recombinant DAGLalpha expressed in African green monkey COS cells using sn-1-stearoyl-2-[14C]-arachidonoyl-glycerol as substrate incubated for 15 mins by beta counting analysis, IC50 = 0.001 μM.	26917221
COS7	Function assay		20 mins	Inhibition of recombinant human HL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.003 μM.	30613337
HT1080	Function assay		20 mins	Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.006 μM.	30613337
HEK293F	Function assay		20 mins	Inhibition of recombinant human PL expressed in HEK293F cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.006 μM.	30613337
HEK293	Function assay	1 uM	10 mins	Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 10 mins by HPLC method, IC50 = 0.01318 μM.	26344596
HEK293	Function assay	1 uM	10 mins	Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 30 mins by HPLC method, IC50 = 0.01413 μM.	26344596
HEK293	Function assay	1 uM	10 mins	Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 60 mins by HPLC method, IC50 = 0.01995 μM.	26344596
N18TG2	Function assay		20 mins	Inhibition of DAGLalpha in mouse N18TG2 cells assessed as inhibition of ionomycin-induced formation of 2-AG incubated for 20 mins by LC-MS analysis, IC50 = 0.02 μM.	26917221
HEK293T	Function assay			Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe, IC50 = 0.03 μM.	18657971
HEK293	Function assay	1 uM	10 mins	Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 90 mins by HPLC method, IC50 = 0.03715 μM.	26344596
HEK293	Function assay			Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells, IC50 = 0.04786 μM.	25752982
HEK293	Function assay			Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells, IC50 = 0.048 μM.	25752982
HEK293T	Function assay			Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe, IC50 = 0.05 μM.	18657971
COS7	Function assay			Inhibition of human recombinant DAGLalpha overexpressed in african green monkey COS7 cells, IC50 = 0.06 μM.	18657971
COS7	Function assay			Inhibition of human recombinant DAGLbeta overexpressed in african green monkey COS7 cells, IC50 = 0.06 μM.	18657971
COS7	Function assay		20 mins	Inhibition of recombinant human LPL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.066 μM.	30613337
HEK293T	Function assay			Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe, IC50 = 0.08 μM.	18657971
HEK293	Function assay			Inhibition of human ABHD12 containing pCMV6-XL4-hABHD12 transfected into HEK293 cells, IC50 = 0.19 μM.	25752982
HEK293	Function assay		10 mins	Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method, IC50 = 0.19 μM.	26344596
HEK293	Function assay			Inhibition of human ABHD12 containing pCMV6-XL4-hABHD12 transfected into HEK293 cells, IC50 = 0.19055 μM.	25752982
HEK293	Function assay		10 mins	Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method, IC50 = 0.19055 μM.	26344596
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells by scintillation counting, Ki = 2.5 μM.	18831576
BxPC3	Function assay		10 to 14 days	Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay, IC50 = 8.45 μM.	25513712
MDA-MB-231	Cytotoxicity assay			Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability, IC50 = 13 μM.	29541373
MDA-MB-435	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay, IC50 = 16.8 μM.	18710210
HepG2 (DPX-2)	Function assay		24 hrs	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50 = 28.2 μM.	20966043
COS7	Function assay			Inhibition of recombinant DAGLbeta overexpressed in african green monkey COS7 cells assessed as accumulation of 2-arachidonoylglycerol by Western blotting	18657971
COS7	Function assay			Inhibition of recombinant DAGLalpha overexpressed in african green monkey COS7 cells assessed as accumulation of 2-arachidonoylglycerol by Western blotting	18657971
MDA-MB-435	Apoptosis assay	25 uM	72 hrs	Induction of apoptosis in human MDA-MB-435 cells assessed as DNA fragmentation at 25 uM after 72 hrs	18710210
HEK293	Function assay	1 uM	10 mins	Reversible inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 10 to 90 mins by HPLC method	26344596
LNCAP	Function assay	20 uM	48 hrs	Induction of cholesterol metabolism deregulation in human LNCAP cells assessed as reduction in NBD-cholesterol uptake at 20 uM after 48 hrs by DAPI/Alexa fluor 633 phalloidin staining based high-content imaging analysis	29474071
BV2	Function assay		30 mins	Inhibition of ABHD6 in mouse BV2 cells preincubated for 30 mins and subsequent addition of [3H]-2-OG substrate measured after 15 mins by liquid scintillation counting method	28284861
BV2	Function assay		30 mins	Inhibition of ABHD12 in mouse BV2 cells preincubated for 30 mins and subsequent addition of [3H]-2-OG substrate measured after 15 mins by liquid scintillation counting method	28284861
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량	495.73	화학식	C₂₉H₅₃NO₅	보관 (수령일로부터)	3년-20°C분말
CAS 번호	96829-58-2	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Tetrahydrolipstatin,Ro 18-0647			Smiles	CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O

용해도 (Solubility)

In vitro
배치:

DMSO : 99 mg/mL (199.7 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 99 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (201.72 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 mg/mL

Water : Insoluble

DMSO : 99 mg/mL (199.7 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 99 mg/mL

Water : Insoluble

DMSO : 99 mg/mL (199.7 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 99 mg/mL

Water : Insoluble

DMSO : 99 mg/mL (199.7 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 99 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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	lipase (Cell-free assay) Fatty acid synthesis (Cell-free assay)
시험관 내(In vitro)	Orlistat, an inhibitor of lipases and fatty acid synthase, is used orally for long-term treatment of obesity. This compound shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein.
생체 내(In vivo)	Orlistat, administered by oral route, is minimally absorbed by the gastrointestinal tract and is able to prevent the absorption of a large percentage of lipids, thereby reducing lipid supply from outside sources. Because of its extremely low oral bioavailability, the effects of this compound are largely confined to the gastrointestinal tract, where it inactivates pancreatic lipase. Therefore, the formulation and route of delivery would have to be changed to treat tumors of the breast, prostate, and so on. This chemical halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice. A pharmacokinetic analysis of this compound (155 mg/kg) administered by i.p. injection showed peak blood levels to be ∼10 μM 2 h after dosing (data not shown). Beyond this time, blood levels of the drug decayed rapidly.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/26035182/ [2] https://pubmed.ncbi.nlm.nih.gov/15026345/

적용 분야 (Applications)

방법	바이오마커	이미지	PMID
Western blot	FASN / AR / p-AKT / p-p53 / p53 / VEGF / Cyclin D1 / Bcl-2 / Cleaved caspase-3		31527721
Growth inhibition assay	Cell viability		28387458

임상시험 정보 (Clinical Trial Information)

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT01755676	Completed	Obesity	EMS	September 2016	Phase 3
NCT02141230	Withdrawn	Weight Loss	GlaxoSmithKline\|Hamell	December 2015	Not Applicable
NCT01719419	Withdrawn	Overweight	Pennington Biomedical Research Center	March 2012	Not Applicable
NCT01332448	Completed	Obesity	GlaxoSmithKline	February 2010	--
NCT01414465	Completed	Overweight	University of Campinas Brazil\|Germed Pharma	October 2009	Not Applicable

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):

Orlistat Lipase 억제제

분자량: 495.73

품질 관리 (Quality Control)

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)

Orlistat Lipase 억제제

분자량: 495.73

품질 관리 (Quality Control)

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)