2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs HMG-CoA Reductase (HMGCR)
  4. PROTAC HMGCR Degrader-1

PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research.

For research use only. We do not sell to patients.

PROTAC HMGCR Degrader-1

PROTAC HMGCR Degrader-1 Chemical Structure

CAS No. : 2715104-45-1

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PROTAC HMGCR Degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research[1].

In Vitro

PROTAC HMGCR Degrader-1 (compound 21 b) is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134) (compound 21 c). PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader degrading HMGCR in Insig-silenced HepG2 cells with DC50 of 120 nM through a VHL-dependent manner [1].
PROTAC HMGCR Degrader-1 (0.01-3 μM, 16 h) preferentially acts as HMGCR inhibitors over degraders at high doses in HepG2 cells, achieves a maximum degradation (Dmax) of 56% at a high dose of 1 μM[1].
PROTAC HMGCR Degrader-1 (1 μM, 16 h) prevents the compensatory upregulation of HMGCR in human hepatic HepG2 cells[1].

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

PROTAC HMGCR Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.01. 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 16 h
Result: Attenuated the upregulation of HMGCR at low concentration.
Increase in HMGCR expression at high concentration.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1 μM
Incubation Time: 16 h
Result: Effectively attenuated the compensatory upregulation of HMGCR.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-24 AUC0-∞
Mice[1] 60 mg/kg p.o. 5.1 h 8.0 h 0.47 μM 5.0 μM 5.4 μM
In Vivo

PROTAC HMGCR Degrader-1 (compound 21 b) (20 or 60 mg/kg. p.o., once a day for 5 weeks) suppress de novo cholesterol synthesis via HMGCR degradation at low dose and exert better effects for promoting excretion of redundant lipids absorbed daily from an MFD27 when cotreat with synergetic statin with well safety profile in medium fat diet (MFD)-induced mouse model[1].

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

Animal Model: MFD (medium-fat containing 12% fat, 0.5% so dium cholate and 1.25% cholesterol) (8 weeks) induced-male C57BL/6 mice (20e24 g)[1]
Dosage: 20 or 60 mg/kg
Administration: p.o., once a day for 5 weeks
Result: Was well tolerated, with no significant change in body weight and food intake.
Demonstrated similar effects to lovastatin.
Decreased total cholesterol (TC), LDL-C and triglyceride (TG) in serum of mice fed on MFD.
Enhanced the reduction in serum lipid levels when combination with lovastatin.
Reduced serum TC and cholesteryl esters to lower levels at a higher dose of 60 mg/kg.
Reduced hepatic TC and TG in a dose-dependent manner.
Ameliorated MFD-induced steatosis and lipid deposition in liver sections.
Induced robust HMGCR degradation at 16 h after final gavage even at a low dose of 20 mg/kg.
Was more effective in lowering total lipids (TC, cholesteryl ester and TG) when cotreated with lovastatin.
Molecular Weight

960.27

Formula

C53H77N5O9S
CAS No.
SMILES

O=C(O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(O3)=O)[C@@]12[H])NCCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC HMGCR Degrader-1 Related Classifications

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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:

PROTAC HMGCR Degrader-12715104-45-1PROTAC HMGCR Degrader1PROTAC HMGCR Degrader 1PROTACsHMG-CoA Reductase (HMGCR)orally activeHMGCRPROTACVHL-dependent mannerhyperlipidemiaInhibitorinhibitorinhibit

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