| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
HUP30 targets multiple components of the vascular signaling pathway to produce vasodilation. The compound stimulates soluble guanylyl cyclase (sGC), the enzyme that catalyzes the conversion of GTP to cyclic GMP (cGMP). cGMP is a second messenger that activates protein kinase G (PKG), which phosphorylates target proteins to promote smooth muscle relaxation and vasodilation. HUP30 also activates K⁺ channels in vascular smooth muscle cells, leading to membrane hyperpolarization. This hyperpolarization closes voltage-gated Ca²⁺ channels, reducing calcium influx and promoting relaxation. Additionally, HUP30 blocks extracellular Ca²⁺ influx, further reducing intracellular calcium levels. This multi-target mechanism of action makes HUP30 a potent vasodilator.
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| ln Vitro |
HUP30 has an IC50 value of 3.9 μM, which inhibits aortic contraction produced by inhibin [1]. Deoxygen-stimulated aortas have higher cGMP levels when exposed to HUP30 (100 μM) [1]. With an IC50 value of 7.5 μM, HUP30 has an antispasmodic effect on arterial aortic rings contracted by 25/30 mM K+[1]. Ca2+ excitation and extracellular Ca2+ influx are induced by HUP30 (3-100 μM) gyro buffer [1]. Single tail artery myocytes' currents are gyroscoped by HUP30 (10-100 μM) [1].
In vitro, HUP30 demonstrates potent vasodilating activity. The compound stimulates soluble guanylyl cyclase, increasing cGMP production in vascular smooth muscle cells. HUP30 activates K⁺ channels, leading to membrane hyperpolarization and reduced excitability. The compound also blocks extracellular Ca²⁺ influx, reducing intracellular calcium levels and promoting smooth muscle relaxation. These combined effects result in potent vasodilation in isolated blood vessel preparations. The compound's multi-target mechanism makes it a valuable tool for studying the regulation of vascular tone and for validating vasodilatory signaling pathways. |
| ln Vivo |
In vivo, HUP30 has been investigated in preclinical models of hypertension and other cardiovascular conditions. As a potent vasodilator, the compound is expected to reduce vascular resistance and lower blood pressure. The compound's multiple mechanisms of action—stimulating sGC, activating K⁺ channels, and blocking Ca²⁺ influx—contribute to its vasodilatory effects. Specific in vivo efficacy data is available from the primary literature describing the compound. The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage in these studies.
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| Enzyme Assay |
The vasodilatory activity of HUP30 is typically assessed using isolated blood vessel preparations in organ baths or using myography. Arterial rings (such as rat aorta or mesenteric arteries) are mounted in organ baths and pre-contracted with vasoconstrictors such as phenylephrine or KCl. Varying concentrations of HUP30 are added, and the relaxation of the arterial rings is measured. The compound's ability to stimulate sGC can be assessed by measuring cGMP levels in vascular tissue or cultured cells using ELISA or RIA. K⁺ channel activation can be assessed using electrophysiological techniques or by using specific K⁺ channel blockers. Ca²⁺ influx blockade can be assessed using fluorescent calcium indicators.
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| Cell Assay |
Cellular assays for HUP30 are performed using vascular smooth muscle cells (such as A7r5 cells or primary smooth muscle cells). Cells are treated with varying concentrations of the compound. Intracellular cGMP levels are measured using ELISA or RIA. Intracellular calcium levels are measured using fluorescent calcium indicators such as Fura-2 or Fluo-4. Membrane potential can be assessed using fluorescent membrane potential-sensitive dyes or patch-clamp electrophysiology. Cell viability and proliferation are assessed using standard assays.
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| Animal Protocol |
In vivo studies of HUP30 are conducted in rodent models of hypertension, such as spontaneously hypertensive rats (SHR) or angiotensin II-infused mice. The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage. Blood pressure is measured using telemetry or tail-cuff methods. Heart rate is monitored. Vascular function is assessed in isolated blood vessels. Pharmacodynamic markers of sGC activation, K⁺ channel activation, and Ca²⁺ channel blockade are assessed in vascular tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HUP30 (molecular weight 305.35, molecular formula C14H15N3O3S) have been characterized. The compound is soluble in DMSO at 20-100 mg/mL. For in vivo administration, the compound is formulated in suitable vehicles. Storage recommendations include powder storage at -20°C for up to 3 years and solution storage at -80°C for 6 months or -20°C for 1 month. Comprehensive PK parameters including oral bioavailability, half-life, and maximum concentration are available from the primary literature.
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| Toxicity/Toxicokinetics |
HUP30 is intended for research use only and is not approved for human therapeutic applications. Comprehensive toxicological evaluations, including acute and repeat-dose toxicity studies in animal models, have been conducted as part of preclinical development. The compound's mechanism of action—vasodilation through sGC stimulation, K⁺ channel activation, and Ca²⁺ channel blockade—may affect blood pressure and cardiovascular function. These effects would be carefully evaluated in toxicology studies. Standard safety pharmacology assessments would include evaluation of effects on cardiovascular function.
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| References | |
| Additional Infomation |
HUP30 is a potent vasodilating agent that stimulates soluble guanylyl cyclase, activates K⁺ channels, and blocks extracellular Ca²⁺ influx. The compound's multi-target mechanism of action—increasing cGMP production, promoting membrane hyperpolarization, and reducing intracellular calcium—results in potent vasodilation. HUP30 is used as a research tool for studying vascular function and blood pressure regulation and for validating vasodilatory signaling pathways as therapeutic targets. The compound has the molecular formula C14H15N3O3S and a molecular weight of 305.35. HUP30 is available with purity ≥98-99% for research use.
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| Molecular Formula |
C14H15N3O3S
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|---|---|
| Molecular Weight |
305.352
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| Exact Mass |
305.083
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| Elemental Analysis |
C, 55.07; H, 4.95; N, 13.76; O, 15.72; S, 10.50
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| CAS # |
312747-21-0
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| PubChem CID |
739510
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| Appearance |
White to light yellow solid powder
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| LogP |
4.896
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
409
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VMAKFFKOZSLHDW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15N3O3S/c18-13(9-4-2-1-3-5-9)16-14-15-11-7-6-10(17(19)20)8-12(11)21-14/h6-9H,1-5H2,(H,15,16,18)
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| Chemical Name |
O=C(C1CCCCC1)NC2=NC3=CC=C([N+]([O-])=O)C=C3S2
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| Synonyms |
HUP30; HUP-30; HUP 30;
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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 : ~100 mg/mL (~327.49 mM )
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2749 mL | 16.3747 mL | 32.7493 mL | |
| 5 mM | 0.6550 mL | 3.2749 mL | 6.5499 mL | |
| 10 mM | 0.3275 mL | 1.6375 mL | 3.2749 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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