1. Immunology/Inflammation
  2. Complement System
  3. FD-IN-1

FD-IN-1 

Cat. No.: HY-128570 Purity: 99.61%
Handling Instructions

FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively.

For research use only. We do not sell to patients.

FD-IN-1 Chemical Structure

FD-IN-1 Chemical Structure

CAS No. : 1646682-14-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively[1].

In Vitro

FD-IN-1 (Compound 12) exhibits functional inhibition of AP activation (IC50=0.26 μM) in vitro in a membrane attack complex (MAC) deposition assay using 50% human whole blood (WB)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

FD-IN-1 (Compound 12) demonstrates systemic suppression of AP activation in a lipopolysaccharide-induced alternative complement pathway (AP) activation model as well as local ocular suppression in intravitreal injection-induced AP activation model in mice expressing human FD[1].
FD-IN-1 (Compound 12) exhibits high oral bioavailability (C57BL6 mice 83%, Beagle dogs 70%) following oral administration (mice and dogs 10 mg/kg)[1].
FD-IN-1 (Compound 12) exhibits terminal elimination half-lives (C57BL6 mice 1.6 h and Beagle dogs 3.8 h) following intravenous administration (mice and dogs 1 mg/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Human FD knock-in mice [1]
Dosage: 3 and 10 mg/kg
Administration: Oral gavage
Result: The AP pathway was fully inhibited for up to 10 h at the 10 mg/kg dose.
Molecular Weight

377.43

Formula

C₂₃H₂₃NO₄

CAS No.
SMILES

O=C(O)CC1=CC=CC=C1OCC2=CC=CC(C3=CC([[email protected]](N)CO)=CC=C3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (165.59 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6495 mL 13.2475 mL 26.4950 mL
5 mM 0.5299 mL 2.6495 mL 5.2990 mL
10 mM 0.2649 mL 1.3247 mL 2.6495 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

FD-IN-1Complement SystemComplementfactor DFDpathwayAPimmunesystemInhibitorinhibitorinhibit

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FD-IN-1
Cat. No.:
HY-128570
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