ALT-946 free base
ALT-946 free base is an orally active inhibitor of the advanced glycation end product (AGE) formation pathway. ALT-946 free base blocks the formation of AGE-protein cross-links, reduces the accumulation of AGE in renal tissues, alleviates increased albuminuria and elevated glomerular filtration rate, prevents glomerulosclerosis, ameliorates medullary tubulointerstitial lesions, and reduces cortical tubular degeneration. ALT-946 free base can be used in research related to diabetic nephropathy and diabetic cardiovascular diseases.
For research use only. We do not sell to patients.
- CAS No.: 727972-45-4
- Formula: C5H13N5O
- Molecular Weight:159.19
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
ALT-946 free base (0.1-30.0 mM) potently inhibits AGE-BSA cross-linking to rat tail tendon collagen in vitro with an IC50 of 3.4 mM[1].
ALT-946 free base potently inhibits AGE-protein cross-linking in an in vitro purified protein system[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
ALT-946 free base (1 g/L; p.o.; daily; 32 weeks or 16 weeks delayed) confers renoprotective effects in streptozotocin-induced diabetic Sprague Dawley rats, including attenuation of hyperfiltration, prevention of albuminuria, and inhibition of glomerular AGE accumulation[1].
ALT-946 free base (1 g/L; p.o.; daily; 12 weeks) confers renoprotection in hypertensive transgenic (mREN-2)27 rats with streptozotocin-induced diabetic nephropathy, reducing albumin excretion rate by 250%, normalizing glomerulosclerosis, improving medullary pathology, and reducing cortical tubular degeneration and renal AGE accumulation without altering blood pressure[3].
ALT-946 free base (1 g/L; p.o.; daily; 12 weeks) has no measurable effect on renal function, histopathology, or AGE levels in healthy nondiabetic transgenic (mREN-2)27 rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis rats (male, ~200 g, streptozotocin-induced diabetic)[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Normalized RBC-IgG levels completely in diabetic rats at 0.03 mg/kg.
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Animal Model:Sprague Dawley rats (male, 200-250 g, streptozotocin-induced diabetic)[1]
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Dosage:1 g/L (continuous 32 weeks); 1 g/L (delayed 16 weeks)
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Administration:p.o.; daily; 32 weeks; p.o.; daily; 16 weeks (delayed from week 16 to 32)
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Result:Did not affect body weight, glycaemic control, or systolic blood pressure in diabetic rats.
Attenuated the diabetes-associated increase in glomerular filtration rate.
Prevented the development of diabetes-associated albuminuria.
Reduced glomerular AGE staining to levels similar to non-diabetic control rats.
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Animal Model:(mREN-2)27 (female, 6 weeks old, streptozotocin-induced diabetic nephropathy)[3]
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Dosage:1 g/L
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Administration:p.o.; daily; 12 weeks
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Result:Reduced the diabetes-induced increase in albumin excretion rate by 250%.
Lowered glomerulosclerotic index to nondiabetic control levels.
Improved medullary tubulointerstitial collagen deposition to a similar extent as aminoguanidine.
Reduced cortical tubular degeneration to a greater degree than aminoguanidine, lowering the number of degenerated tubules per field compared to untreated diabetic rats.
Reduced increased glomerular and tubulointerstitial AGE immunolabeling in diabetic rats to near nondiabetic levels.
Did not alter diabetes-induced increases in kidney weight or glomerular filtration rate.
Did not affect systolic blood pressure or body weight in either nondiabetic or diabetic rats.
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Animal Model:(mREN-2)27 (female, 6 weeks old)[3]
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Dosage:1 g/L
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Administration:p.o.; daily; 12 weeks
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Result:Showed no effect on body weight, kidney weight, systolic blood pressure, glomerular filtration rate, or albumin excretion rate.
Did not alter renal histology, glomerulosclerotic index, cortical tubular morphology, or AGE immunolabeling, all remaining consistent with untreated nondiabetic controls.
Chemical Information
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CAS No. 727972-45-4
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Molecular Weight 159.19
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Formula C5H13N5O
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SMILES
O=C(C)NCCNC(NN)=N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Hepatotoxicity Study
This protocol evaluates hepatotoxicity using complementary in vivo mouse APAP acute liver injury and in vitro hepatocyte-based cytotoxicity readouts. In vivo APAP injury is assessed by serum ALT/AST, liver histology, hepatic glutathione, protein adducts, necrosis, inflammation, and regeneration-related endpoints. In vitro hepatotoxicity is assessed by loss of viability, leakage of ALT/AST/LDH, oxidative-stress markers, mitochondrial function, nuclear morphology, intracellular calcium, and high-content imaging endpoints.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ALT-946 free base Related Classifications
HY-187638A Related Classifications
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Keywords
- ALT-946
- 727972-45-4
- ALT946
- ALT 946
- Biochemical Assay Reagents
- rat tail tendon collagen
- diabetic cardiovascular disease
- streptozotocin-induced diabetic Lewis rats
- renal tissues
- diabetic nephropathy
- glomerulosclerosis
- advanced glycation end-product
- albuminuria
- glomerular filtration rate
- nitric oxide synthase
- Inhibitor
- inhibitor
- inhibit