| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
NorUDCA does not have a specific drug target but acts through multiple mechanisms in the liver. It is a bile acid analog that promotes bile flow (choleresis) and reduces the accumulation of toxic bile acids in the liver. The compound modulates nuclear receptors such as FXR (farnesoid X receptor) and PXR (pregnane X receptor), which regulate bile acid synthesis and transport. It also has anti-inflammatory and anti-fibrotic effects through the inhibition of hepatic stellate cell activation.
|
|---|---|
| ln Vitro |
In preclinical mouse models of cholestatic and fibrotic liver disease, 24-Norucholic Acid, the side-chain-shortened C23 homolog of UDCA, has been demonstrated to be highly efficacious. 24-Norsodeoxycholic acid, in a dose-dependent manner, markedly decreased serum alkaline phosphatase (ALP) levels. Additionally, 24-Norsodeoxycholic acid significantly lowers serum levels of γ-GT, ALT, and AST [1].
NorUDCA demonstrates choleretic, anti-inflammatory, and anti-fibrotic activities in vitro and in vivo. It promotes bile flow by stimulating biliary bicarbonate secretion. The compound reduces the toxicity of hydrophobic bile acids by displacing them from the bile acid pool. It inhibits the activation of hepatic stellate cells, reducing collagen deposition and fibrosis. NorUDCA also has anti-inflammatory effects by reducing the expression of pro-inflammatory cytokines in the liver. |
| ln Vivo |
NorUDCA has been studied in various animal models of liver disease. In rodent models of cholestasis, norUDCA has been shown to improve liver function, reduce bile acid accumulation, and decrease fibrosis. In models of non-alcoholic steatohepatitis (NASH), the compound reduces hepatic steatosis, inflammation, and fibrosis. NorUDCA has also been shown to be effective in animal models of primary biliary cholangitis (PBC) and primary sclerosing cholangitis (PSC).
|
| Enzyme Assay |
The in vitro assay for norUDCA typically involves measuring its effects on bile acid transport and metabolism using hepatocyte cultures or membrane vesicles. The compound's choleretic effects are assessed by measuring biliary bicarbonate secretion. Its anti-inflammatory effects are evaluated by measuring the expression of pro-inflammatory cytokines in cultured hepatocytes or Kupffer cells. Anti-fibrotic effects are assessed by measuring collagen production in hepatic stellate cell cultures.
|
| Cell Assay |
The in vitro cellular assay for norUDCA typically involves culturing hepatocytes, Kupffer cells, or hepatic stellate cells and treating them with varying concentrations of the compound. Cellular responses such as bile acid uptake and efflux, cytokine secretion, collagen production, and cell viability are measured. The compound's effects on nuclear receptor activation (e.g., FXR, PXR) are assessed using reporter gene assays.
|
| Animal Protocol |
In vivo animal studies for norUDCA typically involve the use of rodent models of cholestasis, NASH, or other liver diseases. Animals are administered the compound via oral gavage at various doses. Parameters such as liver function tests (ALT, AST), bile flow, bile acid composition, histopathology, and markers of inflammation and fibrosis are assessed. The compound's therapeutic efficacy is evaluated by comparing treated and control groups.
|
| ADME/Pharmacokinetics |
NorUDCA is orally bioavailable with favorable pharmacokinetic properties. It has a molecular weight of 376.53 g/mol and a molecular formula of C23H38O4. The compound is metabolized in the liver and undergoes enterohepatic circulation. It has a longer half-life than UDCA and shows good liver targeting. The compound is stable and can be formulated for oral administration. Further detailed PK parameters are available from the manufacturer's data sheets.
|
| Toxicity/Toxicokinetics |
NorUDCA has been studied in preclinical and clinical studies and has shown a favorable safety profile. In animal studies, the compound is well tolerated at therapeutic doses. In clinical trials, norUDCA has been evaluated in patients with primary sclerosing cholangitis (PSC) and other cholestatic liver diseases. The compound is generally well tolerated, with mild gastrointestinal side effects reported. It is intended for research use and further clinical development.
|
| References |
[1]. Fickert P, et al. 24-norUrsodeoxycholic acid is superior to ursodeoxycholic acid in the treatment of sclerosing cholangitis in Mdr2 (Abcb4) knockout mice. Gastroenterology. 2006 Feb;130(2):465-81.
|
| Additional Infomation |
Norursodeoxycholic acid is currently being investigated in the clinical trial NCT03872921 (comparison of norursodeoxycholic acid with placebo in the treatment of primary sclerosing cholangitis).
Drug Indications Treatment of autoimmune sclerosing cholangitis, treatment of primary sclerosing cholangitis NorUDCA is a synthetic derivative of ursodeoxycholic acid (UDCA) that has been studied for its potential therapeutic applications in liver diseases. It has choleretic, anti-inflammatory, and anti-fibrotic properties. The compound has been evaluated in clinical trials for primary sclerosing cholangitis (PSC) and other cholestatic liver diseases. It is also being investigated for the treatment of non-alcoholic steatohepatitis (NASH). The compound is intended for research use and further clinical development. |
| Molecular Formula |
C₂₃H₃₈O₄
|
|---|---|
| Molecular Weight |
378.55
|
| Exact Mass |
378.277
|
| CAS # |
99697-24-2
|
| PubChem CID |
192254
|
| Appearance |
White to off-white solid powder
|
| Density |
1.142±0.06 g/cm3 (20 °C, 760 mmHg)
|
| Boiling Point |
536.7±25.0 °C (760 mmHg)
|
| LogP |
4.087
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
591
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@H](CC(O)=O)[C@H]1CC[C@@]2([H])[C@]3([H])[C@@H](O)C[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C
|
| InChi Key |
QYYDXDSPYPOWRO-JHMCBHKWSA-N
|
| InChi Code |
InChI=1S/C23H38O4/c1-13(10-20(26)27)16-4-5-17-21-18(7-9-23(16,17)3)22(2)8-6-15(24)11-14(22)12-19(21)25/h13-19,21,24-25H,4-12H2,1-3H3,(H,26,27)/t13-,14+,15-,16-,17+,18+,19+,21+,22+,23-/m1/s1
|
| Chemical Name |
(3R)-3-[(3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]butanoic acid
|
| Synonyms |
nor-UDCA24-nor-Ursodeoxycholic acid Norucholic acid Norursodeoxycholic Acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~132.08 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.60 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 25.0 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: ≥ 2.5 mg/mL (6.60 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 25.0 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: ≥ 2.5 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6417 mL | 13.2083 mL | 26.4166 mL | |
| 5 mM | 0.5283 mL | 2.6417 mL | 5.2833 mL | |
| 10 mM | 0.2642 mL | 1.3208 mL | 2.6417 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.