| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
XP-23829 targets hydroxycarboxylic acid receptor 2 (HCA2), also known as GPR109A, through its active metabolite monomethyl fumarate. HCA2 is a G protein-coupled receptor involved in anti-inflammatory signaling. By acting as a prodrug, XP-23829 delivers monomethyl fumarate, which activates HCA2 and modulates inflammatory pathways.
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| ln Vitro |
In vitro, XP-23829 is an oral fumaric acid ester that acts as a prodrug of monomethyl fumarate. Its activity is assessed by measuring the conversion to monomethyl fumarate and the subsequent activation of HCA2-mediated signaling pathways. The compound's anti-inflammatory activity is evaluated in cell-based assays measuring cytokine production and inflammatory marker expression.
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| ln Vivo |
In vivo, XP-23829 is used in the research of moderate to severe chronic plaque psoriasis. As an orally bioavailable fumarate ester, it delivers monomethyl fumarate to target tissues. Its efficacy has been demonstrated in preclinical and clinical studies for the treatment of psoriasis.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for XP-23829 are not typically performed, as it is a prodrug that exerts its effects through the active metabolite monomethyl fumarate. Instead, the compound's stability and conversion to monomethyl fumarate are assessed in plasma or tissue homogenates. The active metabolite's activity at HCA2 is measured using receptor binding or functional assays.
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| Cell Assay |
In vitro cellular assays for XP-23829 are performed using immune cells or keratinocytes. Cells are treated with the compound, and the production of inflammatory cytokines (e.g., TNF-α, IL-12, IL-23) is measured by ELISA. The anti-inflammatory activity is quantified by comparing cytokine levels between treated and untreated cells.
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| Animal Protocol |
In vivo animal experiments for XP-23829 are conducted in animal models of psoriasis or other inflammatory skin diseases. A typical protocol involves oral administration of the compound to mice with induced skin inflammation, followed by assessment of skin lesion severity, histological analysis, and measurement of inflammatory markers in skin tissues.
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| ADME/Pharmacokinetics |
XP-23829 has a molecular weight of 243.26 and molecular formula C₁₁H₁₇NO₅. Its chemical name is (N,N-diethylcarbamoyl)methyl methyl (2E)-but-2-ene-1,4-dioate. It is soluble in DMSO and is supplied with purity >98%. It should be stored appropriately to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicological data for XP-23829 are available from studies supporting its development for psoriasis. As a fumaric acid ester, its safety profile is characterized by its effects on the immune system and potential for gastrointestinal side effects. Specific toxicity data are available from regulatory submissions supporting its clinical development.
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| References | |
| Additional Infomation |
XP-23829 is also known as Tepilamide fumarate and PPC-06. It is an orally bioavailable fumaric acid ester prodrug of monomethyl fumarate used in the research of moderate to severe chronic plaque psoriasis. It is a research compound and is not approved for clinical use in all jurisdictions.
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| Molecular Formula |
C11H17NO5
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|---|---|
| Molecular Weight |
243.256383657455
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| Exact Mass |
243.11
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| Elemental Analysis |
C, 54.31; H, 7.04; N, 5.76; O, 32.88
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| CAS # |
1208229-58-6
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| PubChem CID |
46179632
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| Appearance |
White to off-white solid powder
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| LogP |
0.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
17
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)C(=O)COC(=O)/C=C/C(=O)OC
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| InChi Key |
AKUGRXRLHCCENI-VOTSOKGWSA-N
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| InChi Code |
InChI=1S/C11H17NO5/c1-4-12(5-2)9(13)8-17-11(15)7-6-10(14)16-3/h6-7H,4-5,8H2,1-3H3/b7-6+
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| Chemical Name |
4-O-[2-(diethylamino)-2-oxoethyl] 1-O-methyl (E)-but-2-enedioate
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| Synonyms |
XP 23829; XP23829; XP-23829; PPC-06; PPC06; PPC 06
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 125 mg/mL (~513.85 mM)
H2O : ~50 mg/mL (~205.54 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (102.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1108 mL | 20.5541 mL | 41.1083 mL | |
| 5 mM | 0.8222 mL | 4.1108 mL | 8.2217 mL | |
| 10 mM | 0.4111 mL | 2.0554 mL | 4.1108 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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