2. Neuronal Signaling
  3. Amyloid-β
  4. GSK 3039294

GSK 3039294  (Synonyms: GSK294; amyloid P-IN-1)

Cat. No.: HY-19771 Purity: 99.59%
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GSK3039294 is an orally active pro-drug of Miridesap (HY-101861), a circulating serum amyloid P component depleter. GSK3039294 undergoes hydrolysis to form miridesap via a monoester intermediate. GSK3039294 can be used for the research of systemic amyloidosis.

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

GSK 3039294

GSK 3039294 Chemical Structure

CAS No. : 1819986-22-5

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10 mM * 1 mL in DMSO
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GSK 3039294 Related Antibodies

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Description

GSK3039294 is an orally active pro-drug of Miridesap (HY-101861), a circulating serum amyloid P component depleter. GSK3039294 undergoes hydrolysis to form miridesap via a monoester intermediate. GSK3039294 can be used for the research of systemic amyloidosis[1].

In Vitro

GSK3039294 (3 μM; 90 min) exhibits high passive permeability through MDCK-II cell monolayers[1].
GSK3039294 (30.3 ng/mL; 0-30 min) is rapidly hydrolyzed to miridesap in rat, dog, and human liver microsomes[1].

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

GSK 3039294 Related Antibodies
In Vivo

GSK3039294 (3-1000 mg/kg; p.o.; single gavage/repeat gavage for up to 6 months) administered orally to male Han-Wistar rats results in rapid conversion to Miridesap, with equivalent oral bioavailability of miridesap ranging from 30-80% across tested doses and consistent high Miridesap exposure during repeat dosing[1].
GSK3039294 (5-1000 mg/kg; p.o.; repeat gavage for up to 28 days) administered orally to male Marshall beagle dogs results in rapid conversion to miridesap, with an equivalent oral bioavailability of Miridesap of 22% at a 5 mg/kg single dose and consistent high Miridesap exposure during repeat dosing[1].

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

Animal Model: Han-Wistar (male, 10-12 weeks old, 200-250 g)[1]
Dosage: 3-1000 mg/kg (p.o.)
Administration: p.o.; single gavage/repeat gavage for up to 6 months
Result: Achieved equivalent oral bioavailability of miridesap of 56-80% at 3 mg/kg single oral dose, 36-58% at 10 mg/kg single oral dose, 50% at 10 mg/kg single oral dose, 37% at 30 mg/kg single oral dose, and 30% at 100 mg/kg single oral dose.
Showed roughly dose-proportional increases in miridesap exposure and maximum plasma concentration (Cmax) up to 100 mg/kg single oral dose.
Was not detected in rat blood up to 24 hours post-oral administration at any dose, indicating rapid in vivo cleavage to miridesap.
Detected monoester intermediate only at the 100 mg/kg single oral dose, up to 2-4 hours post-administration.
Resulted in consistent high exposure to miridesap with repeat oral doses of 100, 300, and 1000 mg/kg, though exposure was less than dose-proportional at these higher doses.
Animal Model: Marshall beagle (male, at least 10 months old, 6-15 kg)[1]
Dosage: 5 mg/kg (p.o., single); 100-1000 mg/kg (p.o., repeat)
Administration: p.o.; single gavage/repeat gavage for up to 28 days
Result: Achieved equivalent oral bioavailability of miridesap (active metabolite) of 22% at 5 mg/kg single oral dose.
Was not detected in dog blood up to 24 hours post-single oral administration; monoester intermediate was detected up to 2 hours post-administration at very low concentrations.
Resulted in consistent high exposure to miridesap with repeat oral doses of 100, 300, and 1000 mg/kg, though exposure was less than dose-proportional at these higher doses.
Was quantifiable in dog blood during repeat dosing, with exposure increasing with dose and an "intravenous-like" rapid decline, with very low levels detectable up to 24 hours.
Molecular Weight

656.68

Formula

C30H44N2O14
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@H](C(OCOC(OC2CCOCC2)=O)=O)CCC1)CCCCC(N3CCC[C@@H]3C(OCOC(OC4CCOCC4)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (51.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5228 mL 7.6141 mL 15.2281 mL
5 mM 0.3046 mL 1.5228 mL 3.0456 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5228 mL 7.6141 mL 15.2281 mL 38.0703 mL
5 mM 0.3046 mL 1.5228 mL 3.0456 mL 7.6141 mL
10 mM 0.1523 mL 0.7614 mL 1.5228 mL 3.8070 mL
15 mM 0.1015 mL 0.5076 mL 1.0152 mL 2.5380 mL
20 mM 0.0761 mL 0.3807 mL 0.7614 mL 1.9035 mL
25 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5228 mL
30 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2690 mL
40 mM 0.0381 mL 0.1904 mL 0.3807 mL 0.9518 mL
50 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7614 mL
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GSK 3039294 Related Classifications

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  • 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:

GSK 30392941819986-22-5GSK294 amyloid P-IN-1GSK3039294GSK-3039294GSK 294GSK-294Amyloid-ββ-amyloid peptideAβAbetaMDCK-II cell monolayershuman liver microsomesepithelial cell monolayersliver microsomesserum amyloid P componentsystemic amyloidosisintestinal microsomesdogshuman intestinal microsomesmale ratsInhibitorinhibitorinhibit

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