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MedKoo Cat#: 525458 | Name: ORM-3819
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

ORM-3819 is a novel selective and potent inhibitor of PDE III, promoting cardiac contractility through Ca(2+) sensitization. ORM-3819 relaxes isolated porcine coronary arteries.

Chemical Structure

ORM-3819
ORM-3819
CAS#360794-85-0

Theoretical Analysis

MedKoo Cat#: 525458

Name: ORM-3819

CAS#: 360794-85-0

Chemical Formula: C19H19N5O5

Exact Mass: 397.1386

Molecular Weight: 397.39

Elemental Analysis: C, 57.43; H, 4.82; N, 17.62; O, 20.13

Price and Availability

Size Price Availability Quantity
5mg USD 450.00
25mg USD 775.00
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Related CAS #
No Data
Synonym
ORM-3819
IUPAC/Chemical Name
(R)-6-{4-[N'-(4-Hydroxy-3-methoxy-2-nitro-benzylidene)-hydrazino]-phenyl}-5-methyl-4,5-dihydro-2H-pyridazin-3-one
InChi Key
ZGGBTNDTFFNWRD-JZOCJUILSA-N
InChi Code
InChI=1S/C19H19N5O5/c1-11-9-16(26)22-23-17(11)12-3-6-14(7-4-12)21-20-10-13-5-8-15(25)19(29-2)18(13)24(27)28/h3-8,10-11,21,25H,9H2,1-2H3,(H,22,26)/b20-10+/t11-/m1/s1
SMILES Code
O=C1C[C@@H](C)C(C2=CC=C(N/N=C/C3=CC=C(O)C(OC)=C3[N+]([O-])=O)C=C2)=NN1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
ORM-3819 is a novel selective and potent inhibitor of PDE III.
In vitro activity:
ORM-3819 in the concentration range 0.38-230.6 µM evoked concentration-dependent relaxation with a maximum value of 58.1% and an effective concentration of the relaxing substance that caused 50% of maximum relaxation of 72.2 µM. The maximum hyperpolarization produced by ORM-3819 at a concentration of 120 µM (-2.6 ± 0.81 mV, N = 10) did not differ significantly from that induced by C-type natriuretic peptide (CNP), an endogenous hyperpolarizing mediator, at a concentration of 1.4 µM (-3.6 ± 0.38 mV, N = 17). The same effect elicited by the known inodilator levosimendan was less pronounced at a concentration of 3.7 µM: -1.82 ± 0.44 mV, N = 22 (P < 0.05 vs. CNP). The voltage-gated potassium channel inhibitor 4-aminopyridine, at a concentration of 5 mM, attenuated the relaxation induced by ORM-3819 at concentrations of 41.6 or 117.2 µM. These results suggest that ORM-3819 is a potent vasodilating agent able to relieve coronary artery vasospasm by causing hyperpolarization of vascular smooth muscle cells through processes involving activation of voltage-gated potassium channels. Reference: J Cardiovasc Pharmacol. 2019 Sep;74(3):218-224. https://pubmed.ncbi.nlm.nih.gov/31356552/
In vivo activity:
Intravenous administration of ORM-3819 increased LV+dP/dtmax (EC50=0.13±0.05 µM/kg) and improved the rate of LV pressure decrease (-dP/dtmax); (EC50=0.03±0.02 µM/kg) in healthy guinea pigs. In an in vivo dog model of myocardial stunning, ORM-3819 restored the depressed LV+dP/dtmax and improved % segmental shortening (%SS) in the ischemic area (to 18.8±3), which was reduced after the ischaemia-reperfusion insult (from 24.1±2.1 to 11.0±2.4). Reference: Eur J Pharmacol. 2016 Mar 15;775:120-9. https://pubmed.ncbi.nlm.nih.gov/26872993/

Preparing Stock Solutions

The following data is based on the product molecular weight 397.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Márton Z, Pataricza J, Pollesello P, Varró A, Papp JG. The Novel Inodilator ORM-3819 Relaxes Isolated Porcine Coronary Arteries: Role of Voltage-Gated Potassium Channel Activation. J Cardiovasc Pharmacol. 2019 Sep;74(3):218-224. doi: 10.1097/FJC.0000000000000700. Erratum in: J Cardiovasc Pharmacol. 2019 Nov;74(5):481. PMID: 31356552. 2. Nagy L, Pollesello P, Haikala H, Végh Á, Sorsa T, Levijoki J, Szilágyi S, Édes I, Tóth A, Papp Z, Papp JG. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization in combination with selective PDE III inhibition, a novel approach to inotropy. Eur J Pharmacol. 2016 Mar 15;775:120-9. doi: 10.1016/j.ejphar.2016.02.028. Epub 2016 Feb 9. PMID: 26872993.
In vitro protocol:
1. Márton Z, Pataricza J, Pollesello P, Varró A, Papp JG. The Novel Inodilator ORM-3819 Relaxes Isolated Porcine Coronary Arteries: Role of Voltage-Gated Potassium Channel Activation. J Cardiovasc Pharmacol. 2019 Sep;74(3):218-224. doi: 10.1097/FJC.0000000000000700. Erratum in: J Cardiovasc Pharmacol. 2019 Nov;74(5):481. PMID: 31356552.
In vivo protocol:
1. Nagy L, Pollesello P, Haikala H, Végh Á, Sorsa T, Levijoki J, Szilágyi S, Édes I, Tóth A, Papp Z, Papp JG. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization in combination with selective PDE III inhibition, a novel approach to inotropy. Eur J Pharmacol. 2016 Mar 15;775:120-9. doi: 10.1016/j.ejphar.2016.02.028. Epub 2016 Feb 9. PMID: 26872993.
1: Nagy L, Pollesello P, Haikala H, Végh Á, Sorsa T, Levijoki J, Szilágyi S, Édes I, Tóth A, Papp Z, Papp JG. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization in combination with selective PDE III inhibition, a novel approach to inotropy. Eur J Pharmacol. 2016 Mar 15;775:120-9. doi: 10.1016/j.ejphar.2016.02.028. Epub 2016 Feb 9. PubMed PMID: 26872993. 2: Márton Z, Pataricza J, Pollesello P, Varró A, Papp JG. The Novel Inodilator ORM-3819 Relaxes Isolated Porcine Coronary Arteries: Role of Voltage-Gated Potassium Channel Activation. J Cardiovasc Pharmacol. 2019 Sep;74(3):218-224. doi: 10.1097/FJC.0000000000000700. Erratum in: J Cardiovasc Pharmacol. 2019 Nov;74(5):481. doi: 10.1097/FJC.0000000000000756. PMID: 31356552.