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Complement factor D-IN-1 

Cat. No.: HY-102034 Purity: 98.85%
Handling Instructions

Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.

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

Complement factor D-IN-1 Chemical Structure

Complement factor D-IN-1 Chemical Structure

CAS No. : 1386455-76-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 Get quote
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

Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.

IC50 & Target

IC50: 0.006 μM (FD), 0.05 μM (MAC)[1]

In Vitro

The highly specific S1 serine protease factor D (FD) plays a central role in the amplification of the complement alternative pathway (AP) of the innate immune system. Complement factor D-IN-1 (compound 2) shows similar potency against human and monkey FD (IC50s in FD thioesterolytic assays of 0.005 μM and in 50% serum MAC deposition assays of 0.011 μM for both human and monkey)[1].

In Vivo

Complement factor D-IN-1 displays an excellent oral PK profile in Sprague–Dawley rats and, following an oral dose (10 mg/kg) in Brown Norway rats, demonstrates a good distribution and sustained exposure in ocular tissues including the neural retina and the posterior eye cup (PEC), which comprises the sclera, retinal pigmented epithelium, and choroid. Mean exposure levels in plasma, the PEC, and the retina at 6 h after dosing are 0.36, 0.43, and 0.09 μM, respectively[1].

Molecular Weight

483.32

Formula

C₂₁H₁₉BrN₆O₃

CAS No.

1386455-76-0

SMILES

O=C(N)C1=NN(CC(N2[[email protected]](C(NC3=CC=CC(Br)=N3)=O)C[[email protected]@H]4[[email protected]]2C4)=O)C5=C1C=CC=C5

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 : 250 mg/mL (517.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0690 mL 10.3451 mL 20.6902 mL
5 mM 0.4138 mL 2.0690 mL 4.1380 mL
10 mM 0.2069 mL 1.0345 mL 2.0690 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 (4.30 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice[1]

Complement factor D-IN-1 is tested at 30 mg/kg in the human factor D knock-in mouse pharmacodynamic model. Groups of mice (n=4, female human FD knock-in) are treated either with Complement factor D-IN-1 or dosing vehicle by oral gavage at 24, 16, 12, 8, 6, and 4 h, respectively, prior to the termination of the study. All animals are given intraperitoneal LPS to activate complement 7.5 h prior to study termination. Baseline complement levels are obtained from mice that received oral dosing vehicle and intraperitoneal saline (indicated by PBS line on graph). The positive control group receives oral dosing vehicle and intraperitoneal LPS[1].

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

References
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Keywords:

Complement factor D-IN-1OthersInhibitorinhibitorinhibit

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Complement factor D-IN-1
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