N106 free base · Synonyms: N-106 · N 106

N106 is a first-in-class sarcoplasmic reticulum calcium ATPase SUMOylation activator.

For research use only. Not for human or veterinary use.

Target Calcium Channel E1/E2/E3 Enzyme

Research area Cardiovascular Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

N106 structure

CAS No.: 862974-25-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 495.00	BP-02211-100mg	In stock	Get quote
250 mg	USD 980.00	BP-02211-250mg	In stock	Get quote
500 mg	USD 1,560.00	BP-02211-500mg	In stock	Get quote
1 g	USD 2,520.00	BP-02211-1g	In stock	Get quote
2 g	USD 4,050.00	BP-02211-2g	In stock	Get quote

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Description

N106 is a first-in-class sarcoplasmic reticulum calcium ATPase (SERCA2a) SUMOylation activator. N106 directly activates the SUMO-activating enzyme, E1 ligase. N106 can be used for heart failure research[1].

Biological activity

In Vitro N106 treatment increases contractile properties of cultured rat cardiomyocytes. N106 increases cell contractility, calcium-transient SERCA2a's ATPase activity and SUMOylation within 10?min of exposure, and these effects are sustained at 24?h in cardiomyocytes. In Vivo In a murine model, the half-life of N106 is determined to be ～65.4?min with a Cmax of ～2.24?μM when the mice received 10?mg/kg of N106 by intravenous injection. The oral bioavailability (F%) is 56% and 50%, and terminal elimination half-life (t1/2) is 19?min. ? In vivo, N106 (10 mg/kg) increases cardiac SERCA2A SUMOylation, and significantly improves ventricular function in mice with heart failure.

Identifiers

SMILES: COC1=C2C(SC(NC3=NN=C(C4=CC=C(OC)C=C4)O3)=N2)=CC=C1
InChIKey: FBCSWQRNKAYAGY-UHFFFAOYSA-N

Specifications

MW (average): 354.3830
Formula: C₁₇H₁₄N₄O₃S
CAS No.: 862974-25-2
Physical state: Solid
Color: White to off-white
Shipping: 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: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

soluble in DMSO

Documents

References

[1]. Changwon Kho, et al. Small-molecule activation of SERCA2a SUMOylation for the treatment of heart failure. Nat Commun. 2015 Jun 12;6:7229.

Same target

Search Calcium Channel

Same research area

Search Cardiovascular Disease