MedKoo Cat#: 574771 | Name: LDN-27219
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Description:

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

LDN-27219 is a reversible Transglutaminase 2 (TG2) inhibitor that binds at the GTPase site.

Chemical Structure

LDN-27219
LDN-27219
CAS#312946-37-5

Theoretical Analysis

MedKoo Cat#: 574771

Name: LDN-27219

CAS#: 312946-37-5

Chemical Formula: C20H16N4O2S2

Exact Mass: 408.0715

Molecular Weight: 408.49

Elemental Analysis: C, 58.81; H, 3.95; N, 13.72; O, 7.83; S, 15.70

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
50mg USD 1,050.00 2 Weeks
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Related CAS #
No Data
Synonym
LDN 27219; LDN-27219; LDN27219
IUPAC/Chemical Name
2-[(3,4-Dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]acetic acid hydrazide
InChi Key
WLBUICQBNZXIDJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H16N4O2S2/c21-23-16(25)12-28-20-22-18-17(15(11-27-18)13-7-3-1-4-8-13)19(26)24(20)14-9-5-2-6-10-14/h1-11H,12,21H2,(H,23,25)
SMILES Code
O=C(NN)CSC(N1C2=CC=CC=C2)=NC3=C(C(C4=CC=CC=C4)=CS3)C1=O
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
>3 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
Biological target:
LDN-27219 is a reversible, slow-binding inhibitor of TGase.
In vitro activity:
TBD
In vivo activity:
LDN 27219 promoted the closed TG2 conformation and inhibited transamidase activity in mesenteric arteries. LDN 27219 also potentiated acetylcholine-induced relaxation by opening potassium channels in the smooth muscle; these effects were abolished by membrane-permeable TG2 inhibitors promoting the open conformation. In isolated arteries from 35- to 40-week-old rats, transamidase activity was increased, and LDN 27219 improved acetylcholine-induced relaxation more than in younger rats. Reference: Hypertension. 2021 Jan;77(1):216-227. https://pubmed.ncbi.nlm.nih.gov/33249864/
Solvent mg/mL mM
Solubility
DMSO 82.9 203.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 408.49 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. Pinilla E, Comerma-Steffensen S, Prat-Duran J, Rivera L, Matchkov VV, Buus NH, Simonsen U. Transglutaminase 2 Inhibitor LDN 27219 Age-Dependently Lowers Blood Pressure and Improves Endothelium-Dependent Vasodilation in Resistance Arteries. Hypertension. 2021 Jan;77(1):216-227. doi: 10.1161/HYPERTENSIONAHA.120.15352. Epub 2020 Nov 30. PMID: 33249864.
In vitro protocol:
TBD
In vivo protocol:
1. Pinilla E, Comerma-Steffensen S, Prat-Duran J, Rivera L, Matchkov VV, Buus NH, Simonsen U. Transglutaminase 2 Inhibitor LDN 27219 Age-Dependently Lowers Blood Pressure and Improves Endothelium-Dependent Vasodilation in Resistance Arteries. Hypertension. 2021 Jan;77(1):216-227. doi: 10.1161/HYPERTENSIONAHA.120.15352. Epub 2020 Nov 30. PMID: 33249864.