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Chemical Structure| 877636-42-5 Chemical Structure| 877636-42-5

Structure of ML221
CAS No.: 877636-42-5

Chemical Structure| 877636-42-5

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ML221 is a potent apelin receptor (APJ) antagonist with IC50s of 0.70 μM and 1.75 μM in cAMP and β-arrestin assay respectively.

Synonyms: ML221

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Product Details of ML221

CAS No. :877636-42-5
Formula : C17H11N3O6S
M.W : 385.35
SMILES Code : O=C1C=C(CSC2=NC=CC=N2)OC=C1OC(C3=CC=C([N+]([O-])=O)C=C3)=O
Synonyms :
ML221
InChI Key :UASIRTUMPRQVFY-UHFFFAOYSA-N
Pubchem ID :7217941

Safety of ML221

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of ML221

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human hepatic stellate cell lines (HHSteCs) 10 μM 24 hours To evaluate the effect of ML221 on apelin-induced hepatic stellate cell proliferation and activation, results showed that ML221 pretreatment reduced apelin-induced hepatic stellate cell proliferation and activation. PMC9288669
Human primary cholangiocyte cell line (HIBEpiCs) 10 μM 24 hours To evaluate the effect of ML221 on apelin-induced cholangiocyte proliferation, results showed that ML221 pretreatment reduced apelin-induced cholangiocyte proliferation. PMC9288669
TC-1 cells 10 μM 24 hours ML221, a functional antagonist of apelin 13, was used to explore whether MLN protected against lung injury by modulating apelin 13 expression. ML221 inhibited the MLN-induced improvement in cell viability, increased ROS production, and blocked the beneficial effects of MLN on mitochondrial ATP content, cell apoptosis, and senescence. PMC6802616
SG231 cells 10 μM 24 hours ML221 treatment decreased expression of Ki-67, as well as VEGF-A, VEGF-C, Ang-1 and Ang-2 PMC5510601
HuH-28 cells 10 μM 24 hours ML221 treatment significantly decreased expression of Ki-67, as well as VEGF-A, VEGF-C, Ang-1 and Ang-2 PMC5510601
Mz-ChA-1 cells 7.5, 10, 15 μM 24 hours ML221 treatment significantly decreased PCNA and Ki-67 expression PMC5510601
BEnd.3 cells 0-30 μM 24 hours ML221 suppressed endothelial cell proliferation dose-dependently by blocking apelin-APJ signaling without affecting VEGF/VEGFR2 expression. PMC5678128
OVCAR-4 15–50 μM 24–96 hours ML221 suppressed apelin-13-induced cell proliferation. PMC6548659
OVCAR-5 15–50 μM 24–96 hours ML221 efficiently suppressed increased cell proliferation in APJ-overexpressing cells. PMC6548659
HKCI-10 100 µM 3 days Evaluate the effect of ML221 on cell proliferation PMC6691573
HKCI-2 100 µM 3 days Evaluate the effect of ML221 on cell proliferation PMC6691573
PLC5 100 µM 3 days Evaluate the effect of ML221 on cell proliferation PMC6691573
HepG2 100 µM 3 days Evaluate the effect of ML221 on cell proliferation PMC6691573
LO2 100 µM 3 days Evaluate the effect of ML221 on cell proliferation PMC6691573
Buffalo granulosa cells 10 µM 48 hours To evaluate the effect of APLN on E2 and P4 secretion, ML221 significantly reduced the secretion of E2 and P4 PMC8960050
Raji cells 5μM To investigate the effect of apelin/APLNR axis on B cell migration and immune molecule expression. Results showed that apelin/APLNR promoted B cell migration and inflammatory cytokine expression. PMC11659828

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Chronic constriction injury (CCI) model Intrathecal injection 1, 3, 10 and 30 µg Single injection or daily injections for 3 consecutive days To evaluate the effect of ML221 on CCI-induced neuropathic pain. Results showed that ML221 alleviated mechanical allodynia and heat hyperalgesia in a dose-dependent manner. PMC5562064
C57BL/6J mice DOX-induced myocardial injury model Tail vein injection 10 mg/kg Once daily for 7 days To investigate the protective effect of ELA-11 on DOX-induced myocardial injury, results showed that ELA-11 significantly improved cardiac function and reduced myocardial fibrosis and apoptosis. PMC9492932
Mice Diabetic db/db mouse model Intraperitoneal injection 10 mg/kg For 7 consecutive days To evaluate the effect of ML221 on the integrity of the blood-testis barrier and sperm quality in diabetic mice, it was found that ML221 significantly improved the integrity of the blood-testis barrier and improved sperm quality. PMC9705293
Mice Bilateral renal ischemia-reperfusion injury model Intraperitoneal injection 10 mg/kg Administered every other day from the day of the injury until the end of the experiment ML221 blocked the beneficial effects of ELA32 peptide on AKI but had no effect on the combination treatment of nor-NOHA and Paricalcitol PMC10283061
Balb/c nude mice Subcutaneous xenograft model Intraperitoneal injection 10 mg/kg Every other day until the end of the experiment Evaluate the effect of ML221 on HCC xenograft growth PMC6691573
Mice Oxygen-induced retinopathy (OIR) model Intraperitoneal injection 10 mg/kg/day Once daily for 5 days (P12 to P16) ML221 significantly suppressed pathological retinal angiogenesis (reduced neovascular tufts) while promoting revascularization of ischemic areas (reduced avascular area), without altering VEGF/VEGFR2 expression. APJ was highly expressed in abnormal vascular endothelial cells but minimally detected in normal vessels. PMC5678128
Mice Bile duct ligation (BDL) model Tail vein injection 150 μg/kg 3 times per week for 1 week To evaluate the effect of ML221 on bile duct ligation-induced cholangiocyte proliferation and liver fibrosis, results showed that ML221 treatment reduced cholangiocyte proliferation and liver fibrosis. PMC9288669
Nu/nu mice Mz-ChA-1 xenograft model Tail vein injection 150 μg/kg 3 times weekly for 4 weeks ML221 treatment significantly decreased tumor growth PMC5510601
C57BL/6 male mice Bleomycin-induced pulmonary injury model Intraperitoneal injection 150 μg/kg/day Once daily for 3 weeks ML221 was used to block the protective effect of MLN on lung injury by modulating apelin 13. Mice treated with ML221 showed blocked survival benefits induced by MLN and inhibited upregulation of E-cadherin expression. PMC6802616
Mice Myocardial ischemia-reperfusion injury model Langendorff perfusion 50 nM Single dose, 20 minutes To evaluate the protective effects of ML221 on ischemia-reperfusion hearts. Results showed that ML221 treatment partially restored left ventricular function, reduced myocardial infarct size, and synchronized the activation of the PI3K-AKT-mTOR signaling axis. PMC10628527
Sprague-Dawley rats Chronic doxorubicin-induced cardiotoxicity model Subcutaneous administration via osmotic pump 500 µg/kg b.w./day Continuous for 28 days To evaluate the effect of ML221 on doxorubicin-induced electrocardiographic abnormalities. Results showed prolongation of QT and QTc intervals in the ML221 group. PMC11762970

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

12.98mL

2.60mL

1.30mL

25.95mL

5.19mL

2.60mL

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