Seladelpar

SKU: orb1302700

Description

Seladelpar

Research Area

Metabolism Research, Molecular Biology

Images & Validation

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Key Properties

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CAS Number	851528-79-5
MW	444.46
Purity	99.41%
Formula	C₂₁H₂₃F₃O₅S
SMILES	CCO[C@H](COc1ccc(cc1)C(F)(F)F)CSc1ccc(OCC(O)=O)c(C)c1
Target	PPAR
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.25 mM);DMSO:255 mg/mL (573.73 mM)

Bioactivity

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Target IC50	PPARδ:2 nM (EC50)\|PPARα:1600 nM (EC50)
In Vivo	Female Alms1 mutant (foz/foz) mice and their wild-type siblings were subjected to an atherogenic diet for 16 weeks post-weaning. Subsequently, groups (n=8-12) were randomized to receive either 10 mg/kg Seladelpar or a vehicle (1% methylcellulose) via gavage for 8 weeks. Seladelpar efficiently normalized hyperglycemia, hyperinsulinemia, and glucose disposal in foz/foz mice without significantly affecting body weight. It halved serum alanine aminotransferase levels, which ranged from 300-600 U/L in vehicle-treated foz/foz mice, and corrected serum lipid profiles as well as hepatic concentrations of free cholesterol and other lipotoxic lipids elevated in these mice compared to wild-type. These corrections led to the abolition of hepatocyte ballooning and apoptosis, marked reductions in steatosis and liver inflammation, and improved liver fibrosis. Vehicle-treated foz/foz mice had an average nonalcoholic fatty liver disease (NAFLD) activity score of 6.9, indicative of nonalcoholic steatohepatitis (NASH), which Seladelpar entirely reversed (NAFLD activity score reduced to 3.13). In wild-type mice fed an atherogenic diet, Seladelpar administration resulted in an approximate 18% reduction in body weight (P<0.05). However, it had a minimal impact on the body weight of atherogenic diet-fed foz/foz mice. These mice developed severe metabolic disruptions after 16 weeks, which Seladelpar significantly ameliorated (P<0.05). Following an intraperitoneal glucose challenge, blood glucose levels were significantly lower in Seladelpar-treated foz/foz mice compared to vehicle-treated ones (P<0.05), demonstrating Seladelpar's substantial improvement on glucose handling, an effect similarly observed in wild-type mice on an atherogenic diet (P<0.05). Read more...
In Vitro	Seladelpar (MBX-8025) is an orally administered, highly potent (2 nM), and selective PPAR-δ agonist with over 750-fold and 2500-fold specificity over PPAR-α and PPAR-γ receptors, respectively. As a lipid-modifying agent, it effectively improves insulin resistance, diabetes, and atherogenic dyslipidemia by targeting human PPAR-δ at a 50% effective concentration of 2 nM, compared to 1,600 nM for PPAR-α. Read more...
Animal Research	From weaning (week 4), Alms1 mutant (foz/foz) NOD.B10 mice or Wt littermates (female mice in both groups) are fed an atherogenic diet (23% fat, 0.2% cholesterol and 45% simple carbohydrate; 4.78 kcal/g digestible energy) ad libitum for 16 weeks, after which groups are randomized (n=8-12 mice/group) to once-a-day oral administration (by gavage) for 8 weeks of Seladelpar (10 mg/kg in 1% methylcellulose) or vehicle (controls). Animals are housed under 12-hour light/dark cycle and constant temperature of 22°C and receive maximal humane care. Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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diabetes, dyslipidemia, active, atherogenic, Inhibitor, insulin, MBX 8025, MBX8025, MBX-8025, orally, inhibit, Seladelpar, PPARα, PPARδ, PPAR, Peroxisome proliferator-activated receptors, resistance

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Compound Identifiers

PubChem CID

11236126 ↗

Key Properties

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No computed properties available.

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Seladelpar (orb1302700)

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Purity:	>98%
MW:	466.45
Formula:	C₂₁H₂₂F₃NaO₅S

CAS Number:	2751530-13-7
MW:	466.45
Formula:	C₂₁H₂₂F₃NaO₅S

CAS Number:	928821-40-3
MW:	626.68
Formula:	C₂₇H₄₁F₃N₂O₉S

Purity:	>98% (HPLC)
CAS Number:	851528-79-5
MW:	444.5
Formula:	C₂₁H₂₃F₃O₅S

Seladelpar

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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